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Hebei Sankai Chemical Technology Co., Ltd

1. Product advantages High purity, all above 98.5%, no impurities after dissolution We will test each batch to ensure quality OEM and private brand services designed for free Various cap colors available We can also provide MT1 peptide powd

Shanghai Upbio Tech Co.,Ltd

1.No Less 8 years exporting experience. Clients can 100% received goods 2.Lower Price with higher quality 3,Free sample 4,We are sincerely responsible for the "product quality" and "After Service" Upbio is Specialized

LIDE PHARMACEUTICALS LIMITED

Advantage : LIDE PHARMACEUTICALS LTD. is a mid-small manufacturing-type enterprise, engaged in pharmaceutical intermediates of R&D, custom-made and production, and also involving trading chemicals for export. We have established the

Qingdao Beluga Import and Export Co., LTD

(5S,9S,11S,12R)-11-((S)-sec-butyl)-1-(9H-fluoren-9-yl)-5,9-diisopropyl-12-Methoxy-4,10-diMethyl-3,6,8-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid CAS:863971-44-2 Qingdao Belugas Import and Export Co., Ltd. is a scientific and technological comp

Shandong Hanjiang Chemical Co., Ltd.

Hello, dear friend! I'm Hansen and Allen from China. Welcome to my lookchem mall! The following is a brief introduction of our company's products and services. If you are interested in our products, please contact us by emai

Henan Wentao Chemical Product Co., Ltd.

Henan Wentao Chemical Product Co.,Ltd is Located in Zhengzhou High-tech Development Zone with import and export license, We passed ISO 9001:2008 as well, Henan Wentao has developed more than 1000 compounds, which are widely used in the fields of prod

Wuhan Han Sheng New Material Technology Co.,Ltd

Our Advantage: high quality with competitive price High quality standard: BP/USP/EP Enterprise standard All purity customized Fast and safe delivery We have reliable forwarder who can help us deliver our goods more fast and safe. We

Fmoc-3vvd-OH CAS NO.863971-44-2

Cas:863971-44-2

Min.Order:10 Kilogram

Negotiable

Type:Trading Company

inquiry

Zibo Hangyu Biotechnology Development Co., Ltd

Zibo Hangyu Biotechnology Development Co., Ltd is a leading manufacturer and supplier of chemicals in China. We develop produce and distribute high quality pharmaceuticals, intermediates, special chemicals and OLED intermediates and other fine chemi

Xiamen Jenny Chemical Technology Co., Ltd.

GMP standard, high purity, competitive price, in stock 1. Quick Response: within 6 hours after receiving your email. 2. Quality Guarantee: All products are strictly tested by our QC, confirmed by QA, and approved by a third-party lab in China, USA,

EAST CHEMSOURCES LIMITED

factory?direct?saleAppearance:White Powder Storage:Store In Dry, Cool And Ventilated Place Package:25kg/drum, also according to the clients requirement Application:It is widely used as a thickener, emulsifier and stabilizer Transportation:By Sea Or B

Fmoc-3vvd-OH CAS NO.863971-44-2

Cas:863971-44-2

Min.Order:1 Kilogram

FOB Price: $18.0 / 20.0

Type:Trading Company

inquiry

Shandong Mopai Biotechnology Co., LTD

Shandong Mopai Biotechnology Co., LTD is a leading manufacturer and supplier of chemicals in China. We develop produce and distribute high quality pharmaceuticals, intermediates, special chemicals and OLED intermediates and other fine chemicals. W

Fmoc-3vvd-OH CAS NO.863971-44-2

Cas:863971-44-2

Min.Order:1 Gram

Negotiable

Type:Lab/Research institutions

inquiry

KAISA GROUP INC

1.Applied in food field.it can improve the immune system and prolong life. 2.Appliedin cosmetic field.it can improve the skin care. 3.Applied in pharmaceutical field.it can treat various dieases. 4.Our product quality assurance will make our customer

Fmoc-3vvd-OH CAS NO.863971-44-2

Cas:863971-44-2

Min.Order:1 Metric Ton

FOB Price: $1.5

Type:Trading Company

inquiry

SAGECHEM LIMITED

SAGECHEM is a chemical R&D, manufacturing and distribution company in China since 2009, including pharmaceutical intermediates, agrochemical, dyestuff intermediates, organosilicone, API and etc. We also offer a full range of services in custom synthe

SAGECHEM/Tripeptide (MMAE-3)

Cas:863971-44-2

Min.Order:0

Negotiable

Type:Lab/Research institutions

inquiry

Win-Win chemical Co.Ltd

Stock products, own laboratory Package:Grams, Kilograms Application:For R&D Transportation:According to customer request Port:Shanghai

Bluecrystal chem-union

We are a Union of chemistry in China, consists of chemists,engineers, laboratories,factories in China. We organize surplus capacity of R&D and production as well as custom synthesis for chemical products and chemical business project. We are supp

Hangzhou Dingyan Chem Co., Ltd

R & D enterprises have their own stock in stockAppearance:To be subject to the object Package:Customized Application:pharmaceutical intermediates Transportation:Air Port:Shanghai;Guangzhou

Hangzhou J&H Chemical Co., Ltd.

J&H CHEM is one of China's leading providers of integrated fine chemical services including offering, research and development, Custom manufacturing business, as well as other Value-added customer services, for diversified range products of chemicals

Henan Tianfu Chemical Co., Ltd.

1.Our services:A.Supply sampleB.The packing also can be according the customers` requirmentC.Any inquiries will be replied within 24 hoursD.we provide Commerical Invoice, Packing List, Bill of loading, COA , Health certificate and Origin certificate.

Antimex Chemical Limied

Our own factory produces direct sales with absolute price advantage Application:Pharmaceutical industry Transportation:By sea Port:Shanghai/tianjin

Hubei Langyou International Trading Co., Ltd

Fmoc-3vvd-OH CAS NO.863971-44-2 Application:Fmoc-3vvd-OH CAS NO.863971-44-2

Fmoc-3vvd-OH CAS NO.863971-44-2

Cas:863971-44-2

Min.Order:0

Negotiable

Type:Other

inquiry

Wuhan ZeShanCheng Biomedical Technology Co., Ltd.

1,we produce and sell good chemicals around the world. 2,our success rate is about 95%. this means, if customer order is accepted, the probability that the customer will obtain the ordered substances, is 95%. 3,our staff consists of highl

Henan Kanbei Chemical Co.,LTD

factory?direct?saleAppearance:White powder Storage:Sealed and preserved Package:200/Kilograms Application:healing drugs Transportation:By sea Port:Shanghai/tianjin

Hebei Quanhe Biotechnology Co. LTD

1. Timely and efficient service to ensure communication with customers2. Produce products of different specifications and sizes according to your requirements.3. Quality procedures and standards recognized by SGS. Advanced plant equipment ensures sta

Shanghai Chinqesen Biotechnology Co., Ltd.

Good Quality Package:1kg/bag Application:Medical or chemical Transportation:Air/Train/Sea Port:Shenzhen

863971-44-2

Cas:863971-44-2

Min.Order:0

Negotiable

Type:Trading Company

inquiry

Hunan Longxianng Runhui Trading Co.,Ltd

Fmoc-3vvd-OH CAS NO.863971-44-2Appearance:powder crystal Storage:Keep in dry and cool place Package:Jinbo with Application:used in medical research Transportation:By express (Door to door) such as FEDEX, DHL, EMS for small amount. By air(airport to a

Fmoc-3vvd-OH CAS NO.863971-44-2

Cas:863971-44-2

Min.Order:0

Negotiable

Type:Lab/Research institutions

inquiry

Shanghai Yuanye Bio-Technology Co., Ltd.

good quality, competitive price, thoughtful after sale serviceAppearance:white powder Storage:Keep it in dry,shady and cool place Package:500mg Application:Pharma;Industry;Agricultural;chemical reaserch Transportation:by express or by sea Port:Any po

Saiwante (shanghai) New Material Technology Co., Ltd.

Stable supply of goods and provision of high-quality services Application:As raw materials in the field of medicine and biology

Fmoc-3vvd-OH CAS NO.863971-44-2

Cas:863971-44-2

Min.Order:0

Negotiable

Type:Trading Company

inquiry

Synthetic route

tert-butyl (5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H-fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oate
474645-25-5

tert-butyl (5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H-fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oate

(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid
863971-44-2

(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid

Conditions
ConditionsYield
With trifluoroacetic acid In dichloromethane at 20℃; for 2h;86%
With trifluoroacetic acid In dichloromethane
With trifluoroacetic acid In dichloromethane
(3R,4S,5S)-4-[(2S)-2-[[(9H-fluoren-9-ylmethoxy)carbonyl]amino]-N,3-dimethylbutanamido]-3-methoxy-5-methylheptanoate
177423-00-6

(3R,4S,5S)-4-[(2S)-2-[[(9H-fluoren-9-ylmethoxy)carbonyl]amino]-N,3-dimethylbutanamido]-3-methoxy-5-methylheptanoate

(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid
863971-44-2

(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; benzotriazol-1-ol / N,N-dimethyl-formamide / 20 °C
2: trifluoroacetic acid / dichloromethane / 2 h / 20 °C
View Scheme
Multi-step reaction with 2 steps
1: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; benzotriazol-1-ol / N,N-dimethyl-formamide / 20 °C
2: trifluoroacetic acid / dichloromethane / 2 h / 20 °C
View Scheme
Multi-step reaction with 2 steps
1: N-ethyl-N,N-diisopropylamine; diethyl dicarbonate / ethyl acetate / 20 °C
2: trifluoroacetic acid / dichloromethane / 20 °C
View Scheme
tert-Butyl (3R,4S,5S)-3-methoxy-4-(N-methylamino)-5-methylheptanoate
474645-22-2

tert-Butyl (3R,4S,5S)-3-methoxy-4-(N-methylamino)-5-methylheptanoate

(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid
863971-44-2

(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid

Conditions
ConditionsYield
Multi-step reaction with 4 steps
1: 2-bromo-1-ethylpyridin-1-ium tetrafluoroborate; N-ethyl-N,N-diisopropylamine / dichloromethane / 20 h / -10 - 20 °C
2: palladium 10% on activated carbon; hydrogen / methanol / 1 h / 20 °C
3: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; benzotriazol-1-ol / N,N-dimethyl-formamide / 20 °C
4: trifluoroacetic acid / dichloromethane / 2 h / 20 °C
View Scheme
Multi-step reaction with 4 steps
1: N-ethyl-N,N-diisopropylamine; 2-bromo-1-ethylpyridinium tetrafluoroborate / dichloromethane / 20 h / -10 - 20 °C
2: palladium 10% on activated carbon; hydrogen / methanol / 1 h / 20 °C
3: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; benzotriazol-1-ol / N,N-dimethyl-formamide / 20 °C
4: trifluoroacetic acid / dichloromethane / 2 h / 20 °C
View Scheme
(S)-N-(benzyloxycarbonyl)valine
1149-26-4

(S)-N-(benzyloxycarbonyl)valine

(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid
863971-44-2

(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid

Conditions
ConditionsYield
Multi-step reaction with 4 steps
1: 2-bromo-1-ethylpyridin-1-ium tetrafluoroborate; N-ethyl-N,N-diisopropylamine / dichloromethane / 20 h / -10 - 20 °C
2: palladium 10% on activated carbon; hydrogen / methanol / 1 h / 20 °C
3: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; benzotriazol-1-ol / N,N-dimethyl-formamide / 20 °C
4: trifluoroacetic acid / dichloromethane / 2 h / 20 °C
View Scheme
Multi-step reaction with 4 steps
1: N-ethyl-N,N-diisopropylamine; 2-bromo-1-ethylpyridinium tetrafluoroborate / dichloromethane / 20 h / -10 - 20 °C
2: palladium 10% on activated carbon; hydrogen / methanol / 1 h / 20 °C
3: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; benzotriazol-1-ol / N,N-dimethyl-formamide / 20 °C
4: trifluoroacetic acid / dichloromethane / 2 h / 20 °C
View Scheme
tert-butyl (3R,4S,5S)-4-[(2S)-2-[[(benzyloxy)carbonyl]amino]-N,3-dimethylbutanamido]-3-methoxy-5-methylheptanoate
120205-52-9

tert-butyl (3R,4S,5S)-4-[(2S)-2-[[(benzyloxy)carbonyl]amino]-N,3-dimethylbutanamido]-3-methoxy-5-methylheptanoate

(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid
863971-44-2

(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1: palladium 10% on activated carbon; hydrogen / methanol / 1 h / 20 °C
2: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; benzotriazol-1-ol / N,N-dimethyl-formamide / 20 °C
3: trifluoroacetic acid / dichloromethane / 2 h / 20 °C
View Scheme
Multi-step reaction with 3 steps
1: palladium 10% on activated carbon; hydrogen / methanol / 1 h / 20 °C
2: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; benzotriazol-1-ol / N,N-dimethyl-formamide / 20 °C
3: trifluoroacetic acid / dichloromethane / 2 h / 20 °C
View Scheme
Fmoc-Val-OH
68858-20-8

Fmoc-Val-OH

(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid
863971-44-2

(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid

Conditions
ConditionsYield
Multi-step reaction with 4 steps
1: 2-chloro-4,6-dimethoxy-1 ,3,5-triazine / 20 °C
2: diethylamine / tetrahydrofuran / 20 °C
3: N-ethyl-N,N-diisopropylamine; diethyl dicarbonate / ethyl acetate / 20 °C
4: trifluoroacetic acid / dichloromethane / 20 °C
View Scheme
tert-butyl (3R,4S,5S)-4-[(2S)-2-[[(9H-fluoren-9-ylmethoxy)carbonyl]amino]-N,3-dimethylbutanamido]-3-methoxy-5-methylheptanoate
1375415-93-2

tert-butyl (3R,4S,5S)-4-[(2S)-2-[[(9H-fluoren-9-ylmethoxy)carbonyl]amino]-N,3-dimethylbutanamido]-3-methoxy-5-methylheptanoate

(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid
863971-44-2

(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1: diethylamine / tetrahydrofuran / 20 °C
2: N-ethyl-N,N-diisopropylamine; diethyl dicarbonate / ethyl acetate / 20 °C
3: trifluoroacetic acid / dichloromethane / 20 °C
View Scheme
tert-Butyl (3R,4S,5S)-3-methoxy-4-(N-methylamino)-5-methylheptanoate hydrochloride
120205-48-3

tert-Butyl (3R,4S,5S)-3-methoxy-4-(N-methylamino)-5-methylheptanoate hydrochloride

(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid
863971-44-2

(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid

Conditions
ConditionsYield
Multi-step reaction with 4 steps
1: 2-chloro-4,6-dimethoxy-1 ,3,5-triazine / 20 °C
2: diethylamine / tetrahydrofuran / 20 °C
3: N-ethyl-N,N-diisopropylamine; diethyl dicarbonate / ethyl acetate / 20 °C
4: trifluoroacetic acid / dichloromethane / 20 °C
View Scheme
(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid
863971-44-2

(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid

(2R,3R)-3-methoxy-2-methyl-N-[(2S)-1-(1,2-oxazinan-2-yl)-1-oxo-3-phenylpropan-2-yl]-3-[(2S)-pyrrolidin-2-yl]propanamide, trifluoroacetic acid salt
1352201-70-7

(2R,3R)-3-methoxy-2-methyl-N-[(2S)-1-(1,2-oxazinan-2-yl)-1-oxo-3-phenylpropan-2-yl]-3-[(2S)-pyrrolidin-2-yl]propanamide, trifluoroacetic acid salt

N-[(9H-fluoren-9-ylmethoxy)carbonyl]-N-methyl-L-valyl-N-[(3R,4S,5S)-3-methoxy-1-{(2S)-2-[(1R,2R)-1-methoxy-2-methyl-3-{[(2S)-1-(1,2-oxazinan-2-yl)-1-oxo-3-phenylpropan-2-yl]amino}-3-oxopropyl]pyrrolidin-1-yl}-5-methyl-1-oxoheptan-4-yl]-N-methyl-L-valinamide

N-[(9H-fluoren-9-ylmethoxy)carbonyl]-N-methyl-L-valyl-N-[(3R,4S,5S)-3-methoxy-1-{(2S)-2-[(1R,2R)-1-methoxy-2-methyl-3-{[(2S)-1-(1,2-oxazinan-2-yl)-1-oxo-3-phenylpropan-2-yl]amino}-3-oxopropyl]pyrrolidin-1-yl}-5-methyl-1-oxoheptan-4-yl]-N-methyl-L-valinamide

Conditions
ConditionsYield
With N-ethyl-N,N-diisopropylamine; HATU In N,N-dimethyl-formamide at 20℃; for 3h;100%
With N-ethyl-N,N-diisopropylamine; N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate In N,N-dimethyl-formamide at 20℃; for 3h;100%
(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid
863971-44-2

(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid

(2R,3R)-3-methoxy-2-methyl-N-[(2S,3S)-1-(1,2-oxazinan-2-yl)-1-oxo-3-phenylbutan-2-yl]-3-[(2S)-pyrrolidin-2-yl]propanamide, trifluoroacetic acid salt
1352201-95-6

(2R,3R)-3-methoxy-2-methyl-N-[(2S,3S)-1-(1,2-oxazinan-2-yl)-1-oxo-3-phenylbutan-2-yl]-3-[(2S)-pyrrolidin-2-yl]propanamide, trifluoroacetic acid salt

N-[(9H-fluoren-9-ylmethoxy)carbonyl]-N-methyl-L-valyl-N-[(3R,4S,5S)-3-methoxy-1-{(2S)-2-[(1R,2R)-1-methoxy-2-methyl-3-{[(2S,3S)-1-(1,2-oxazinan-2-yl)-1-oxo-3-phenylbutan-2-yl]amino}-3-oxopropyl]pyrrolidin-1-yl}-5-methyl-1-oxoheptan-4-yl]-N-methyl-L-valinamide

N-[(9H-fluoren-9-ylmethoxy)carbonyl]-N-methyl-L-valyl-N-[(3R,4S,5S)-3-methoxy-1-{(2S)-2-[(1R,2R)-1-methoxy-2-methyl-3-{[(2S,3S)-1-(1,2-oxazinan-2-yl)-1-oxo-3-phenylbutan-2-yl]amino}-3-oxopropyl]pyrrolidin-1-yl}-5-methyl-1-oxoheptan-4-yl]-N-methyl-L-valinamide

Conditions
ConditionsYield
With benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; N-ethyl-N,N-diisopropylamine In N,N-dimethyl-formamide at 20℃;100%
With benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; N-ethyl-N,N-diisopropylamine In N,N-dimethyl-formamide at 20℃;100%
(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid
863971-44-2

(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid

(2R,3R)-3-methoxy-2-methyl-N-[(2S)-1-(2-oxa-3-azabicyclo[2.2.2]oct-5-en-3-yl)-1-oxo-3-phenylpropan-2-yl]-3-[(2S)-pyrrolidin-2-yl]propanamide trifluoroacetate

(2R,3R)-3-methoxy-2-methyl-N-[(2S)-1-(2-oxa-3-azabicyclo[2.2.2]oct-5-en-3-yl)-1-oxo-3-phenylpropan-2-yl]-3-[(2S)-pyrrolidin-2-yl]propanamide trifluoroacetate

N-[(9H-fluoren-9-ylmethoxy)carbonyl]-N-methyl-L-valyl-N-[(3R,4S,5S)-3-methoxy-1-{(2S)-2-[(1R,2R)-1-methoxy-2-methyl-3-{[(2S)-1-(2-oxa-3-azabicyclo[2.2.2]oct-5-en-3-yl)-1-oxo-3-phenylpropan-2-yl]amino}-3-oxopropyl]pyrrolidin-1-yl}-5-methyl-1-oxoheptan-4-yl]-N-methyl-L-valinamide

N-[(9H-fluoren-9-ylmethoxy)carbonyl]-N-methyl-L-valyl-N-[(3R,4S,5S)-3-methoxy-1-{(2S)-2-[(1R,2R)-1-methoxy-2-methyl-3-{[(2S)-1-(2-oxa-3-azabicyclo[2.2.2]oct-5-en-3-yl)-1-oxo-3-phenylpropan-2-yl]amino}-3-oxopropyl]pyrrolidin-1-yl}-5-methyl-1-oxoheptan-4-yl]-N-methyl-L-valinamide

Conditions
ConditionsYield
With N-ethyl-N,N-diisopropylamine; HATU In N,N-dimethyl-formamide at 20℃; for 1h;98%
With N-ethyl-N,N-diisopropylamine; N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate In N,N-dimethyl-formamide at 20℃; for 1h;98%
(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid
863971-44-2

(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid

di-tert-butyl dicarbonate
24424-99-5

di-tert-butyl dicarbonate

N-(tert-butoxycarbonyl)-N-methyl-L-valyl-N-[(2R,3S,4S)-1-carboxy-2-methoxy-4-methylhexan-3-yl]-N-methyl-L-valinamide

N-(tert-butoxycarbonyl)-N-methyl-L-valyl-N-[(2R,3S,4S)-1-carboxy-2-methoxy-4-methylhexan-3-yl]-N-methyl-L-valinamide

Conditions
ConditionsYield
Stage #1: (5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H-fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid With piperidine In N,N-dimethyl-formamide at 20℃; for 0.166667h;
Stage #2: di-tert-butyl dicarbonate In 1,4-dioxane; water pH=11;
97%
(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid
863971-44-2

(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid

dap-phe-OMe hydrochloride salt

dap-phe-OMe hydrochloride salt

C55H77N5O10

C55H77N5O10

Conditions
ConditionsYield
With diethyl cyanophosphonate; N-ethyl-N,N-diisopropylamine In dichloromethane for 1h;87%
(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid
863971-44-2

(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid

(x)C2HF3O2*C25H40N2O7

(x)C2HF3O2*C25H40N2O7

C61H89N5O13

C61H89N5O13

Conditions
ConditionsYield
With diethyl cyanophosphonate; N-ethyl-N,N-diisopropylamine In dichloromethane at 20℃; for 2h;81%
(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid
863971-44-2

(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid

(S)-tert-butyl 2-((2R,3R)-3-methoxy-2-methyl-3-((2S,5S)-5-methylpyrrolidin-2-yl)propanamido)-3-phenylpropanoate

(S)-tert-butyl 2-((2R,3R)-3-methoxy-2-methyl-3-((2S,5S)-5-methylpyrrolidin-2-yl)propanamido)-3-phenylpropanoate

(S)-tert-butyl 2-((2R,3R)-3-((2S,5S)-1-((5S,8S,11S,12R)-11-sec-butyl-1-(9H-fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecane)-5-methylpyrrolidin-2-yl)-3-methoxy-2-methylpropanamido)-3-phenylpropanoate

(S)-tert-butyl 2-((2R,3R)-3-((2S,5S)-1-((5S,8S,11S,12R)-11-sec-butyl-1-(9H-fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecane)-5-methylpyrrolidin-2-yl)-3-methoxy-2-methylpropanamido)-3-phenylpropanoate

Conditions
ConditionsYield
With N-ethyl-N,N-diisopropylamine; N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate In dichloromethane; N,N-dimethyl-formamide at 20 - 30℃; for 1h; Inert atmosphere;81%
(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid
863971-44-2

(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid

(S)-2,4-dimethoxybenzyl 2-((2R,3R)-3-((1S,3S,5S)-2-azabicyclo[3.1.0]hexan-3-yl)-3-methoxy-2-methylpropanamido)-3-(2-fluorophenyl)propanoate

(S)-2,4-dimethoxybenzyl 2-((2R,3R)-3-((1S,3S,5S)-2-azabicyclo[3.1.0]hexan-3-yl)-3-methoxy-2-methylpropanamido)-3-(2-fluorophenyl)propanoate

(S)-2,4-dimethoxybenzyl 2-((2R,3R)-3-((1S,3S,5S)-2-((5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H-fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oyl)-2-azabicyclo[3.1.0]hexan-3-yl)-3-methoxy-2-methylpropanamido)-3-(2-fluorophenyl)propanoate

(S)-2,4-dimethoxybenzyl 2-((2R,3R)-3-((1S,3S,5S)-2-((5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H-fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oyl)-2-azabicyclo[3.1.0]hexan-3-yl)-3-methoxy-2-methylpropanamido)-3-(2-fluorophenyl)propanoate

Conditions
ConditionsYield
With N-ethyl-N,N-diisopropylamine; HATU In dichloromethane; N,N-dimethyl-formamide at 20℃; for 1h; Temperature; Solvent; Inert atmosphere;75.8%
(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid
863971-44-2

(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid

(2R,3R)-3-methoxy-2-methyl-N-[(1S)-2-phenyl-1-(1,3-thiazol-2-yl)ethyl]-3-[(2S)-pyrrolidin-2-yl]propanethioamide, trifluoroacetic acid salt
1438851-45-6

(2R,3R)-3-methoxy-2-methyl-N-[(1S)-2-phenyl-1-(1,3-thiazol-2-yl)ethyl]-3-[(2S)-pyrrolidin-2-yl]propanethioamide, trifluoroacetic acid salt

N-[(9H-fluoren-9-ylmethoxy)carbonyl]-N-methyl-L-valyl-N-[(3R,4S,5S)-3-methoxy-1-{(2S)-2-[(1R,2R)-1-methoxy-2-methyl-3-{[(1S)-2-phenyl-1-(1,3-thiazol-2-yl)ethyl]amino}-3-thioxopropyl]pyrrolidin-1-yl}-5-methyl-1-oxoheptan-4-yl]-N-methyl-L-valinamide

N-[(9H-fluoren-9-ylmethoxy)carbonyl]-N-methyl-L-valyl-N-[(3R,4S,5S)-3-methoxy-1-{(2S)-2-[(1R,2R)-1-methoxy-2-methyl-3-{[(1S)-2-phenyl-1-(1,3-thiazol-2-yl)ethyl]amino}-3-thioxopropyl]pyrrolidin-1-yl}-5-methyl-1-oxoheptan-4-yl]-N-methyl-L-valinamide

Conditions
ConditionsYield
With triethylamine; HATU In dichloromethane; N,N-dimethyl-formamide75%
(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid
863971-44-2

(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid

benzyl N-{(2R,3R)-3-methoxy-2-methyl-3-[(2S)-pyrrolidin-2-yl]propanoyl}-L-phenylalaninate trifluoroacetate
1369426-89-0

benzyl N-{(2R,3R)-3-methoxy-2-methyl-3-[(2S)-pyrrolidin-2-yl]propanoyl}-L-phenylalaninate trifluoroacetate

N-[(9H-fluoren-9-ylmethoxy)carbonyl]-N-methyl-L-valyl-N-[(3R,4S,5S)-1-{(2S)-2-[(1R,2R)-3-{[(2S)-1-(benzyloxy)-1-oxo-3-phenylpropan-2-yl]amino}-1-methoxy-2-methyl-3-oxopropyl]pyrrolidin-1-yl}-3-methoxy-5-methyl-1-oxoheptan-4-yl]-N-methyl-L-valinamide

N-[(9H-fluoren-9-ylmethoxy)carbonyl]-N-methyl-L-valyl-N-[(3R,4S,5S)-1-{(2S)-2-[(1R,2R)-3-{[(2S)-1-(benzyloxy)-1-oxo-3-phenylpropan-2-yl]amino}-1-methoxy-2-methyl-3-oxopropyl]pyrrolidin-1-yl}-3-methoxy-5-methyl-1-oxoheptan-4-yl]-N-methyl-L-valinamide

Conditions
ConditionsYield
With benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; N-ethyl-N,N-diisopropylamine In N,N-dimethyl-formamide at 20℃;68%
With benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; N-ethyl-N,N-diisopropylamine In N,N-dimethyl-formamide at 20℃;68%
(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid
863971-44-2

(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid

(2R,3R)-3-methoxy-2-methyl-N-(2-phenylethyl)-3-[(2S)-pyrrolidin-2-yl]propanethioamide hydrochloride

(2R,3R)-3-methoxy-2-methyl-N-(2-phenylethyl)-3-[(2S)-pyrrolidin-2-yl]propanethioamide hydrochloride

N-[(9H-fluoren-9-ylmethoxy)carbonyl]-N-methyl-L-valyl-N-{(3R,4S,5S)-3-methoxy-[(2S)-2-{(1R,2R)-methoxy-2-methyl-3-[(2-phenylethyl)amino]-3-thioxopropyl}pyrrolidin-1-yl]-5-methyl-1-oxoheptan-4-yl}-N-methyl-L-valinamide

N-[(9H-fluoren-9-ylmethoxy)carbonyl]-N-methyl-L-valyl-N-{(3R,4S,5S)-3-methoxy-[(2S)-2-{(1R,2R)-methoxy-2-methyl-3-[(2-phenylethyl)amino]-3-thioxopropyl}pyrrolidin-1-yl]-5-methyl-1-oxoheptan-4-yl}-N-methyl-L-valinamide

Conditions
ConditionsYield
With N-ethyl-N,N-diisopropylamine; HATU In dichloromethane; N,N-dimethyl-formamide for 2h;66%
(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid
863971-44-2

(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid

(S)-tert-butyl 2-((2R,3R)-3-((1S,3S,5S)-2-azabicyclo[3.1.0]hexan-3-yl)-3-methoxy-2-methylpropanamido)-3-phenylpropanoate

(S)-tert-butyl 2-((2R,3R)-3-((1S,3S,5S)-2-azabicyclo[3.1.0]hexan-3-yl)-3-methoxy-2-methylpropanamido)-3-phenylpropanoate

(S)-tert-butyl 2-((2R,3R)-3-((1S,3S,5S)-2-((5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(1H-fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-yl)-2-azabicyclo[3.1.0]hexan-3-yl)-3-methoxy-2-methylpropanamido)-3-phenylpropanoate

(S)-tert-butyl 2-((2R,3R)-3-((1S,3S,5S)-2-((5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(1H-fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-yl)-2-azabicyclo[3.1.0]hexan-3-yl)-3-methoxy-2-methylpropanamido)-3-phenylpropanoate

Conditions
ConditionsYield
With N-ethyl-N,N-diisopropylamine; N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate In dichloromethane; N,N-dimethyl-formamide at 20 - 30℃; for 1h; Inert atmosphere;54.9%
(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid
863971-44-2

(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid

(2R,3R)-3-methoxy-2-methyl-3-[(2S)-pyrrolidin-2-yl]propanoic acid trifluoroacetate

(2R,3R)-3-methoxy-2-methyl-3-[(2S)-pyrrolidin-2-yl]propanoic acid trifluoroacetate

N-[(9H-fluoren-9-ylmethoxy)carbonyl]-N-methyl-L-valyl-N-[(3R,4S,5S)-1-{(2S)-2-[(1R,2R)-2-carboxy-1-methoxypropyl]pyrrolidin-1-yl}-3-methoxy-5-methyl-1-oxoheptan-4-yl]-N-methyl-L-valinamide

N-[(9H-fluoren-9-ylmethoxy)carbonyl]-N-methyl-L-valyl-N-[(3R,4S,5S)-1-{(2S)-2-[(1R,2R)-2-carboxy-1-methoxypropyl]pyrrolidin-1-yl}-3-methoxy-5-methyl-1-oxoheptan-4-yl]-N-methyl-L-valinamide

Conditions
ConditionsYield
With benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; N-ethyl-N,N-diisopropylamine In N,N-dimethyl-formamide at 20℃; for 3.5h;35%
Stage #1: (5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H-fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid With benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In N,N-dimethyl-formamide at 20℃; for 1.5h;
Stage #2: (2R,3R)-3-methoxy-2-methyl-3-[(2S)-pyrrolidin-2-yl]propanoic acid trifluoroacetate With N-ethyl-N,N-diisopropylamine In N,N-dimethyl-formamide at 20℃; for 2h;
35%
1-hydroxy-pyrrolidine-2,5-dione
6066-82-6

1-hydroxy-pyrrolidine-2,5-dione

(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid
863971-44-2

(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid

Fmoc-MeVal-Val-Dil-OSu
920017-35-2

Fmoc-MeVal-Val-Dil-OSu

Conditions
ConditionsYield
With dicyclohexyl-carbodiimide In tetrahydrofuran at 20℃; for 48h;
(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid
863971-44-2

(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid

C37H37Cl2N2O4Pol

C37H37Cl2N2O4Pol

C73H86Cl2N5O10Pol

C73H86Cl2N5O10Pol

Conditions
ConditionsYield
With N-ethyl-N,N-diisopropylamine; HATU In N,N-dimethyl-formamide for 6h; not specified;
(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid
863971-44-2

(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid

(2R,3R)-3-methoxy-2-methyl-N-[(1S)-2-phenyl-1-(1,3-thiazol-2-yl)ethyl]-3-[(2S)-pyrrolidin-2-yl]propanethioamide, trifluoroacetic acid salt
1438851-45-6

(2R,3R)-3-methoxy-2-methyl-N-[(1S)-2-phenyl-1-(1,3-thiazol-2-yl)ethyl]-3-[(2S)-pyrrolidin-2-yl]propanethioamide, trifluoroacetic acid salt

N-methyl-L-valyl-N-[(3R,4S,5S)-3-methoxy-1-{(2S)-2-[(1R,2R)-1-methoxy-2-methyl-3-{[(1S)-2-phenyl-1-(1,3-thiazol-2-yl)ethyl]amino}-3-thioxopropyl]pyrrolidin-1-yl}-5-methyl-1-oxoheptan-4-yl]-N-methyl-L-valinamide

N-methyl-L-valyl-N-[(3R,4S,5S)-3-methoxy-1-{(2S)-2-[(1R,2R)-1-methoxy-2-methyl-3-{[(1S)-2-phenyl-1-(1,3-thiazol-2-yl)ethyl]amino}-3-thioxopropyl]pyrrolidin-1-yl}-5-methyl-1-oxoheptan-4-yl]-N-methyl-L-valinamide

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1: HATU; triethylamine / dichloromethane; N,N-dimethyl-formamide
2: diethylamine / dichloromethane
View Scheme
(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid
863971-44-2

(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid

N-(tert-butoxycarbonyl)-N-methyl-L-valyl-N-[(3R,4S,5S)-1-{(2S)-2-[(1R,2R)-3-{[(2S)-1-(benzyloxy)-3-phenylpropan-2-yl]amino}-1-methoxy-2-methyl-3-oxopropyl]pyrrolidin-1-yl}-3-methoxy-5-methyl-1-oxoheptan-4-yl]-N-methyl-L-valinamide

N-(tert-butoxycarbonyl)-N-methyl-L-valyl-N-[(3R,4S,5S)-1-{(2S)-2-[(1R,2R)-3-{[(2S)-1-(benzyloxy)-3-phenylpropan-2-yl]amino}-1-methoxy-2-methyl-3-oxopropyl]pyrrolidin-1-yl}-3-methoxy-5-methyl-1-oxoheptan-4-yl]-N-methyl-L-valinamide

Conditions
ConditionsYield
Multi-step reaction with 4 steps
1.1: piperidine / N,N-dimethyl-formamide / 0.17 h / 20 °C
1.2: pH 11
2.1: HATU; N-ethyl-N,N-diisopropylamine / N,N-dimethyl-formamide / 5 h / 20 °C
3.1: palladium 10% on activated carbon; hydrogen / dichloromethane; methanol / 0.5 h / 20 °C
4.1: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; benzotriazol-1-ol; N-ethyl-N,N-diisopropylamine / N,N-dimethyl-formamide / 0.5 h / 20 °C
View Scheme
Multi-step reaction with 5 steps
1: piperidine / N,N-dimethyl-formamide / 0.17 h / 20 °C
2: sodium hydroxide / 1,4-dioxane; water / pH 11
3: N-ethyl-N,N-diisopropylamine; N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate / N,N-dimethyl-formamide / 0.08 h / 20 °C
4: palladium 10% on activated carbon; hydrogen / dichloromethane; methanol / 0.5 h / 20 °C
5: N-ethyl-N,N-diisopropylamine; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; benzotriazol-1-ol / N,N-dimethyl-formamide / 0.5 h / 20 °C
View Scheme
(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid
863971-44-2

(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid

N-methyl-L-valyl-N-[(3R,4S,5S)-1-{(2S)-2-[(1R,2R)-3-{[(2S)-1-(benzyloxy)-3-phenylpropan-2-yl]amino}-1-methoxy-2-methyl-3-oxopropyl]pyrrolidin-1-yl}-3-methoxy-5-methyl-1-oxoheptan-4-yl]-N-methyl-L-valinamide trifluoroacetate

N-methyl-L-valyl-N-[(3R,4S,5S)-1-{(2S)-2-[(1R,2R)-3-{[(2S)-1-(benzyloxy)-3-phenylpropan-2-yl]amino}-1-methoxy-2-methyl-3-oxopropyl]pyrrolidin-1-yl}-3-methoxy-5-methyl-1-oxoheptan-4-yl]-N-methyl-L-valinamide trifluoroacetate

Conditions
ConditionsYield
Multi-step reaction with 5 steps
1.1: piperidine / N,N-dimethyl-formamide / 0.17 h / 20 °C
1.2: pH 11
2.1: HATU; N-ethyl-N,N-diisopropylamine / N,N-dimethyl-formamide / 5 h / 20 °C
3.1: palladium 10% on activated carbon; hydrogen / dichloromethane; methanol / 0.5 h / 20 °C
4.1: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; benzotriazol-1-ol; N-ethyl-N,N-diisopropylamine / N,N-dimethyl-formamide / 0.5 h / 20 °C
5.1: dichloromethane / 0.5 h / 20 °C
View Scheme
Multi-step reaction with 6 steps
1: piperidine / N,N-dimethyl-formamide / 0.17 h / 20 °C
2: sodium hydroxide / 1,4-dioxane; water / pH 11
3: N-ethyl-N,N-diisopropylamine; N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate / N,N-dimethyl-formamide / 0.08 h / 20 °C
4: palladium 10% on activated carbon; hydrogen / dichloromethane; methanol / 0.5 h / 20 °C
5: N-ethyl-N,N-diisopropylamine; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; benzotriazol-1-ol / N,N-dimethyl-formamide / 0.5 h / 20 °C
6: dichloromethane / 0.5 h / 20 °C
View Scheme
(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid
863971-44-2

(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid

[3H]-Vedotin
474645-27-7

[3H]-Vedotin

Conditions
ConditionsYield
Multi-step reaction with 5 steps
1.1: piperidine / N,N-dimethyl-formamide / 0.17 h / 20 °C
1.2: pH 11
2.1: HATU; N-ethyl-N,N-diisopropylamine / N,N-dimethyl-formamide / 5 h / 20 °C
3.1: palladium 10% on activated carbon; hydrogen / dichloromethane; methanol / 0.5 h / 20 °C
4.1: HATU; N-ethyl-N,N-diisopropylamine / N,N-dimethyl-formamide / 0.08 h / 20 °C
5.1: trifluoroacetic acid / dichloromethane
View Scheme
Multi-step reaction with 6 steps
1: piperidine / N,N-dimethyl-formamide / 0.17 h / 20 °C
2: sodium hydroxide / 1,4-dioxane; water / pH 11
3: N-ethyl-N,N-diisopropylamine; N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate / N,N-dimethyl-formamide / 0.08 h / 20 °C
4: palladium 10% on activated carbon; hydrogen / dichloromethane; methanol / 0.5 h / 20 °C
5: N-ethyl-N,N-diisopropylamine; N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate / N,N-dimethyl-formamide / 0.08 h / 20 °C
6: dichloromethane
View Scheme
Multi-step reaction with 2 steps
1: N-ethyl-N,N-diisopropylamine; N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate / N,N-dimethyl-formamide; dichloromethane / 20 °C
2: diethylamine / dichloromethane / 20 °C
View Scheme
(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid
863971-44-2

(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid

C44H75N5O9

C44H75N5O9

Conditions
ConditionsYield
Multi-step reaction with 4 steps
1.1: piperidine / N,N-dimethyl-formamide / 0.17 h / 20 °C
1.2: pH 11
2.1: HATU; N-ethyl-N,N-diisopropylamine / N,N-dimethyl-formamide / 5 h / 20 °C
3.1: palladium 10% on activated carbon; hydrogen / dichloromethane; methanol / 0.5 h / 20 °C
4.1: HATU; N-ethyl-N,N-diisopropylamine / N,N-dimethyl-formamide / 0.08 h / 20 °C
View Scheme
Multi-step reaction with 5 steps
1: piperidine / N,N-dimethyl-formamide / 0.17 h / 20 °C
2: sodium hydroxide / 1,4-dioxane; water / pH 11
3: N-ethyl-N,N-diisopropylamine; N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate / N,N-dimethyl-formamide / 0.08 h / 20 °C
4: palladium 10% on activated carbon; hydrogen / dichloromethane; methanol / 0.5 h / 20 °C
5: N-ethyl-N,N-diisopropylamine; N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate / N,N-dimethyl-formamide / 0.08 h / 20 °C
View Scheme
(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid
863971-44-2

(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid

(S)-2-((2R,3R)-3-((S)-1-((6S,9S,12S,13R)-12-((S)-sec-butyl)-6,9-diisopropyl-13-methoxy-2,2,5,11-tetramethyl-4,7,10-trioxo-3-oxa-5,8,11-triazapentadecan-15-oyl)pyrrolidin-2-yl)-3-methoxy-2-methylpropanamido)-3-phenylpropanoic acid
1369427-27-9

(S)-2-((2R,3R)-3-((S)-1-((6S,9S,12S,13R)-12-((S)-sec-butyl)-6,9-diisopropyl-13-methoxy-2,2,5,11-tetramethyl-4,7,10-trioxo-3-oxa-5,8,11-triazapentadecan-15-oyl)pyrrolidin-2-yl)-3-methoxy-2-methylpropanamido)-3-phenylpropanoic acid

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1.1: piperidine / N,N-dimethyl-formamide / 0.17 h / 20 °C
1.2: pH 11
2.1: HATU; N-ethyl-N,N-diisopropylamine / N,N-dimethyl-formamide / 0.17 h / 20 °C
3.1: palladium 10% on activated carbon; hydrogen / methanol
View Scheme
Multi-step reaction with 4 steps
1: piperidine / N,N-dimethyl-formamide / 0.17 h / 20 °C
2: sodium hydroxide / 1,4-dioxane; water / pH 11
3: N-ethyl-N,N-diisopropylamine; N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate / N,N-dimethyl-formamide / 0.17 h / 20 °C
4: palladium 10% on activated carbon; hydrogen / methanol / 1 h / 20 °C
View Scheme
(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid
863971-44-2

(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid

C51H79N5O10

C51H79N5O10

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1.1: piperidine / N,N-dimethyl-formamide / 0.17 h / 20 °C
1.2: pH 11
2.1: HATU; N-ethyl-N,N-diisopropylamine / N,N-dimethyl-formamide / 0.17 h / 20 °C
View Scheme
Multi-step reaction with 3 steps
1: piperidine / N,N-dimethyl-formamide / 0.17 h / 20 °C
2: sodium hydroxide / 1,4-dioxane; water / pH 11
3: N-ethyl-N,N-diisopropylamine; N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate / N,N-dimethyl-formamide / 0.17 h / 20 °C
View Scheme
(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid
863971-44-2

(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid

N-(tert-butoxycarbonyl)-N-methyl-L-valyl-N-[(3R,4S,5S)-3-methoxy-1-{(2S)-2-[(1R,2R)-1-methoxy-2-methyl-3-oxo-3-{[(1S)-2-phenyl-1-(5-phenyl-1,3,4-oxadiazol-2-yl)ethyl]amino}propyl]pyrrolidin-1-yl}-5-methyl-1-oxoheptan-4-yl]-N-methyl-L-valinamide

N-(tert-butoxycarbonyl)-N-methyl-L-valyl-N-[(3R,4S,5S)-3-methoxy-1-{(2S)-2-[(1R,2R)-1-methoxy-2-methyl-3-oxo-3-{[(1S)-2-phenyl-1-(5-phenyl-1,3,4-oxadiazol-2-yl)ethyl]amino}propyl]pyrrolidin-1-yl}-5-methyl-1-oxoheptan-4-yl]-N-methyl-L-valinamide

Conditions
ConditionsYield
Multi-step reaction with 4 steps
1.1: piperidine / N,N-dimethyl-formamide / 0.17 h / 20 °C
1.2: pH 11
2.1: HATU; N-ethyl-N,N-diisopropylamine / N,N-dimethyl-formamide / 5 h / 20 °C
3.1: palladium 10% on activated carbon; hydrogen / dichloromethane; methanol / 0.5 h / 20 °C
4.1: HATU; N-ethyl-N,N-diisopropylamine / N,N-dimethyl-formamide / 20 °C
View Scheme
Multi-step reaction with 5 steps
1.1: piperidine / N,N-dimethyl-formamide / 0.17 h / 20 °C
2.1: sodium hydroxide / 1,4-dioxane; water / pH 11
3.1: N-ethyl-N,N-diisopropylamine; N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate / N,N-dimethyl-formamide / 0.08 h / 20 °C
4.1: palladium 10% on activated carbon; hydrogen / dichloromethane; methanol / 0.5 h / 20 °C
5.1: N-ethyl-N,N-diisopropylamine; N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate / N,N-dimethyl-formamide / 0.5 h / 20 °C
5.2: 20 °C
View Scheme
(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid
863971-44-2

(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid

N-methyl-L-valyl-N-[(3R,4S,5S)-3-methoxy-1-{(2S)-2-[(1R,2R)-1-methoxy-2-methyl-3-oxo-3-{[(1S)-2-phenyl-1-(5-phenyl-1,3,4-oxadiazol-2-yl)ethyl]amino}propyl]pyrrolidin-1-yl}-5-methyl-1-oxoheptan-4-yl]-N-methyl-L-valinamide trifluoroacetate

N-methyl-L-valyl-N-[(3R,4S,5S)-3-methoxy-1-{(2S)-2-[(1R,2R)-1-methoxy-2-methyl-3-oxo-3-{[(1S)-2-phenyl-1-(5-phenyl-1,3,4-oxadiazol-2-yl)ethyl]amino}propyl]pyrrolidin-1-yl}-5-methyl-1-oxoheptan-4-yl]-N-methyl-L-valinamide trifluoroacetate

Conditions
ConditionsYield
Multi-step reaction with 5 steps
1.1: piperidine / N,N-dimethyl-formamide / 0.17 h / 20 °C
1.2: pH 11
2.1: HATU; N-ethyl-N,N-diisopropylamine / N,N-dimethyl-formamide / 5 h / 20 °C
3.1: palladium 10% on activated carbon; hydrogen / dichloromethane; methanol / 0.5 h / 20 °C
4.1: HATU; N-ethyl-N,N-diisopropylamine / N,N-dimethyl-formamide / 20 °C
View Scheme
(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid
863971-44-2

(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid

N-(3-carboxypropyl)-N-methyl-L-valyl-N-[(3R,4S,5S)-3-methoxy-1-{(2S)-2-[(1R,2R)-1-methoxy-2-methyl-3-{[(1S,2R)-1-(1,2-oxazinan-2-ylcarbonyl)-2-phenylcyclopropyl]amino}-3-oxopropyl]pyrrolidin-1-yl}-5-methyl-1-oxoheptan-4-yl]-N-methyl-L-valinamide

N-(3-carboxypropyl)-N-methyl-L-valyl-N-[(3R,4S,5S)-3-methoxy-1-{(2S)-2-[(1R,2R)-1-methoxy-2-methyl-3-{[(1S,2R)-1-(1,2-oxazinan-2-ylcarbonyl)-2-phenylcyclopropyl]amino}-3-oxopropyl]pyrrolidin-1-yl}-5-methyl-1-oxoheptan-4-yl]-N-methyl-L-valinamide

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1: HATU; N-ethyl-N,N-diisopropylamine / N,N-dimethyl-formamide / 2 h / 20 °C
2: piperidine / N,N-dimethyl-formamide / 0.5 h / 20 °C
3: sodium cyanoborohydride; hydrogenchloride / 1,4-dioxane; water / 6 h / 100 °C / pH 3
View Scheme
Multi-step reaction with 3 steps
1.1: N-ethyl-N,N-diisopropylamine; N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate / N,N-dimethyl-formamide / 2 h / 20 °C
2.1: piperidine / N,N-dimethyl-formamide / 0.5 h / 20 °C
3.1: 1,4-dioxane; water / 1 h / 100 °C
3.2: 20 - 100 °C / pH 3
View Scheme
(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid
863971-44-2

(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid

N-(5-carboxypentyl)-N-methyl-L-valyl-N-[(3R,4S,5S)-3-methoxy-1-{(2S)-2-[(1R,2R)-1-methoxy-2-methyl-3-{[(1S,2R)-1-(1,2-oxazinan-2-ylcarbonyl)-2-phenylcyclopropyl]amino}-3-oxopropyl]pyrrolidin-1-yl}-5-methyl-1-oxoheptan-4-yl]-N-methyl-L-valinamide

N-(5-carboxypentyl)-N-methyl-L-valyl-N-[(3R,4S,5S)-3-methoxy-1-{(2S)-2-[(1R,2R)-1-methoxy-2-methyl-3-{[(1S,2R)-1-(1,2-oxazinan-2-ylcarbonyl)-2-phenylcyclopropyl]amino}-3-oxopropyl]pyrrolidin-1-yl}-5-methyl-1-oxoheptan-4-yl]-N-methyl-L-valinamide

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1: HATU; N-ethyl-N,N-diisopropylamine / N,N-dimethyl-formamide / 2 h / 20 °C
2: piperidine / N,N-dimethyl-formamide / 0.5 h / 20 °C
3: sodium cyanoborohydride; hydrogenchloride / 1,4-dioxane; water / 4 h / 100 °C / pH 3
View Scheme
Multi-step reaction with 3 steps
1.1: N-ethyl-N,N-diisopropylamine; N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate / N,N-dimethyl-formamide / 2 h / 20 °C
2.1: piperidine / N,N-dimethyl-formamide / 0.5 h / 20 °C
3.1: 1,4-dioxane; water / 1 h / 100 °C
3.2: 20 - 100 °C / pH 3
View Scheme
(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid
863971-44-2

(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid

N-(3-carboxypropyl)-N-methyl-L-valyl-N-[(3R,4S,5S)-1-{(2S)-2-[(1R,2R)-3-{[(2S)-1-(adamantan-1-ylmethoxy)-1-oxo-3-phenylpropan-2-yl]amino}-1-methoxy-2-methyl-3-oxopropyl]pyrrolidin-1-yl}-3-methoxy-5-methyl-1-oxoheptan-4-yl]-N-methyl-L-valinamide

N-(3-carboxypropyl)-N-methyl-L-valyl-N-[(3R,4S,5S)-1-{(2S)-2-[(1R,2R)-3-{[(2S)-1-(adamantan-1-ylmethoxy)-1-oxo-3-phenylpropan-2-yl]amino}-1-methoxy-2-methyl-3-oxopropyl]pyrrolidin-1-yl}-3-methoxy-5-methyl-1-oxoheptan-4-yl]-N-methyl-L-valinamide

Conditions
ConditionsYield
Multi-step reaction with 6 steps
1.1: piperidine / N,N-dimethyl-formamide / 0.17 h / 20 °C
1.2: pH 11
2.1: HATU; N-ethyl-N,N-diisopropylamine / N,N-dimethyl-formamide / 5 h / 20 °C
3.1: palladium 10% on activated carbon; hydrogen / dichloromethane; methanol / 0.5 h / 20 °C
4.1: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; benzotriazol-1-ol; N-ethyl-N,N-diisopropylamine / N,N-dimethyl-formamide / 20 °C
5.1: dichloromethane / 0.5 h
6.1: sodium cyanoborohydride; hydrogenchloride / 1,4-dioxane; water / 5 h / 100 °C
View Scheme
Multi-step reaction with 7 steps
1.1: piperidine / N,N-dimethyl-formamide / 0.17 h / 20 °C
2.1: sodium hydroxide / 1,4-dioxane; water / pH 11
3.1: N-ethyl-N,N-diisopropylamine; N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate / N,N-dimethyl-formamide / 0.08 h / 20 °C
4.1: palladium 10% on activated carbon; hydrogen / dichloromethane; methanol / 0.5 h / 20 °C
5.1: N-ethyl-N,N-diisopropylamine; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; benzotriazol-1-ol / N,N-dimethyl-formamide / 0.5 h / 20 °C
6.1: dichloromethane / 0.5 h
7.1: 1,4-dioxane; water / 1 h / 100 °C
7.2: 4 h / 100 °C / pH 3
View Scheme
(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid
863971-44-2

(5S,8S,11S,12R)-11-((S)-sec-butyl)-1-(9H fluoren-9-yl)-5,8-diisopropyl-12-methoxy-4,10-dimethyl-3,6,9-trioxo-2-oxa-4,7,10-triazatetradecan-14-oic acid

N-(3-carboxypropyl)-N-methyl-L-valyl-N-[(3R,4S,5S)-1-{(2S)-2-[(1R,2R)-3-{[(2S)-1-(benzyloxy)-3-phenylpropan-2-yl]amino}-1-methoxy-2-methyl-3-oxopropyl]pyrrolidin-1-yl}-3-methoxy-5-methyl-1-oxoheptan-4-yl]-N-methyl-L-valinamide

N-(3-carboxypropyl)-N-methyl-L-valyl-N-[(3R,4S,5S)-1-{(2S)-2-[(1R,2R)-3-{[(2S)-1-(benzyloxy)-3-phenylpropan-2-yl]amino}-1-methoxy-2-methyl-3-oxopropyl]pyrrolidin-1-yl}-3-methoxy-5-methyl-1-oxoheptan-4-yl]-N-methyl-L-valinamide

Conditions
ConditionsYield
Multi-step reaction with 6 steps
1.1: piperidine / N,N-dimethyl-formamide / 0.17 h / 20 °C
1.2: pH 11
2.1: HATU; N-ethyl-N,N-diisopropylamine / N,N-dimethyl-formamide / 5 h / 20 °C
3.1: palladium 10% on activated carbon; hydrogen / dichloromethane; methanol / 0.5 h / 20 °C
4.1: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; benzotriazol-1-ol; N-ethyl-N,N-diisopropylamine / N,N-dimethyl-formamide / 0.5 h / 20 °C
5.1: dichloromethane / 0.5 h / 20 °C
6.1: sodium cyanoborohydride; hydrogenchloride / 1,4-dioxane; water / 5 h / 100 °C
View Scheme
Multi-step reaction with 7 steps
1.1: piperidine / N,N-dimethyl-formamide / 0.17 h / 20 °C
2.1: sodium hydroxide / 1,4-dioxane; water / pH 11
3.1: N-ethyl-N,N-diisopropylamine; N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate / N,N-dimethyl-formamide / 0.08 h / 20 °C
4.1: palladium 10% on activated carbon; hydrogen / dichloromethane; methanol / 0.5 h / 20 °C
5.1: N-ethyl-N,N-diisopropylamine; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; benzotriazol-1-ol / N,N-dimethyl-formamide / 0.5 h / 20 °C
6.1: dichloromethane / 0.5 h / 20 °C
7.1: 1,4-dioxane; water / 1 h / 100 °C
7.2: 4 h / 100 °C / pH 3
View Scheme

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