We are concentrating on APIs and pharmaceutical intermediates. With in depth knowledge and understanding in this industry, we are indulged in supplying a wide assortments of 7,10-Dimethoxy 10-DAB III from Wuhan, Hubei, China. It is made obtaina
Cas:114915-14-9
Min.Order:1 Kilogram
FOB Price: $4.8 / 5.0
Type:Trading Company
inquiryAs a leading manufacturer and supplier of chemicals in China, DayangChem not only supply popular chemicals, but also DayangChem's R&D center offer custom synthesis services. DayangChem can provide different quantities of custom synthesis ch
Cas:114915-14-9
Min.Order:1 Kilogram
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Type:Lab/Research institutions
inquiryUnique advantages of Docetaxel intermediate Cas 114915-14-9 Guaranteed purity High quality & competitive price Quality control Fast feedback Prompt shipment Appearance:White powder Storage:Cool dry place Package:100g,1kg/foil bag
Cas:114915-14-9
Min.Order:100 Gram
Negotiable
Type:Trading Company
inquiryProduct Name: Docetaxel intermediate Synonyms: DOCETAXEL INTERMEDIATE;INTERMEDIATE FOR DOCETAXEL;IntermediateIIIforDocetaxel;INTERMEDIATEOFDOCETAXEL;N-1 Step intermediate;(aR,bS)-beta-[[(1,1-Dimethylethoxy)carbonyl]amino]-alpha-hydroxy
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Min.Order:1 Gram
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Type:Lab/Research institutions
inquiryWITH US,YOUR MONEY IN SAFE,YOUR BUSINESS IN SAFE 1)Quick Response Within 12 hours; 2)Quality Guarantee: All products are strictly tested by our QC, confirmed by QA and approved by third party lab in China, USA, Canada, Germany, UK, Italy, France et
Cas:114915-14-9
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Type:Trading Company
inquiryAdvantage : 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 R&
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Negotiable
Type:Lab/Research institutions
inquiry1. 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 ♦ W
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Type:Trading Company
inquiryOur advantages: 1. All inquiries will be replied within 12 hours. 2. Dedication to quality, supply & service. 3. Strictly on selecting raw materials. 4. Reasonable & competitive price, fast lead time. 5. Sample is available for your eva
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Type:Trading Company
inquiry1.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
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Min.Order:1 Kilogram
Negotiable
Type:Lab/Research institutions
inquiryProduct Name: Docetaxel intermediate Synonyms: 7,10-Di Troc Docetaxel;Docetaxel InterMediate (N-1);Benzenepropanoic acid, b-[[(1,1-diMethylethoxy)carbonyl]aMino]-a-hydroxy-,(2aR,4S,4aS,6R,9S,11S,12S,12aR,12bS)-12b-(acetyloxy)-12-(benzoyloxy)-2a
Cas:114915-14-9
Min.Order:1 Gram
Negotiable
Type:Lab/Research institutions
inquiryDocetaxel intermediate CAS:114915-14-9 Qingdao Belugas Import and Export Co., Ltd. is a scientific and technological company integrating research and development, production and trade of chemical intermediates, specializing in high quality organic i
Cas:114915-14-9
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Negotiable
Type:Lab/Research institutions
inquiryHello, 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
Cas:114915-14-9
Min.Order:1 Kilogram
Negotiable
Type:Lab/Research institutions
inquiryPRODUCT DETAILS
Cas:114915-14-9
Min.Order:500 Kilogram
FOB Price: $1.0 / 2.0
Type:Lab/Research institutions
inquiryHenan 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
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inquiryTriumph has the complete production of G- KG - MT service chain,we can make the new technology into productivity quickly in the research and development of new products. Main Service 1.Own made fine chemical products 2.Out sourcing and qua
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inquiryOur company provides one-stop services of research - development - production for a variety of special prouducts. Not only do we make effective use of our strong technological strength, but also establish of cooperative relations with several well-
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Negotiable
Type:Lab/Research institutions
inquiryCompany Introduction 1. Established in 2005, with two independent business divisions: Fine chemicals division; Pharmaceutical division. 2. Main product: Optical brightener Textile auxiliary Dye stuff Pigments
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Min.Order:1 Gram
Negotiable
Type:Lab/Research institutions
inquiryJ&H CHEM R&D center can offer custom synthesis according to the contract research and development services for the fine chemicals, pharmaceutical, biotechnique and some of the other chemicals. J&H CHEM has some Manufacturing base in Jia
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inquiry1.high purity 2.consistent quality 3.competitive price 4.fast shipping Binbo Biological Products Co. Ltd., is a professional high-tech enterprise which engaged in Biological products raw materials. Binbo is engaged in R&D with perfect equipm
Cas:114915-14-9
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inquirystocks High quaiity Appearance:White Storage:Preserve In Well-Closed, Light-Resistant and Tight Containers. Store In Cool & Dry Place Package:1g,5g,10g...1kg,5kg...more Application:API Transportation:shipping,land,air Port:Shanghai
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Min.Order:1 Gram
Negotiable
Type:Lab/Research institutions
inquiryZibo 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
Cas:114915-14-9
Min.Order:10 Gram
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Type:Lab/Research institutions
inquiryThe above product is Ality Chemical's strong item with best price, good quality and fast supply. Ality Chemical has been focusing on the research and production of this field for over 14 years. At the same time, we are always committed to providing h
Superior quality, moderate price & quick delivery. Appearance:powder Storage:Stored in cool, dry and ventilation place; Away from fire and heat Package:1kg/bag, 1kg/drum or 25kg/drum or as per your request. Application:Used in organic synthesis
Lyander’s R&D center can offer custom synthesis according to the contract research and development services for the fine chemicals, pharmaceutical, biotechnique and some of the other chemicals. Lyander can provide different quantities of cu
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Min.Order:1 Gram
Negotiable
Type:Lab/Research institutions
inquiryProduct name: Docetaxel Protective Matter CAS No.:114915-14-9 Molecule Formula:C49H55Cl6NO18 Molecule Weight:1158.67 Purity: 98.0% Package: 25kg/drum Description:White powder Manufacture Standards:Enterprise Standard
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Min.Order:1 Kilogram
Negotiable
Type:Trading Company
inquiryProduct Details Grade: pharmaceutical grade Purity:99%+ ProductionCapacity: 1000 Kilogram/Month Scope of use: For scientific research only(The product must be used legally) Our Advantage 1. Best quality with competitive price. 2. Quick shipping,
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Min.Order:1 Kilogram
Negotiable
Type:Lab/Research institutions
inquiryShandong 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
Cas:114915-14-9
Min.Order:1 Gram
Negotiable
Type:Lab/Research institutions
inquiryWuhu Nuovo Chemical Technology Co., Ltd. was established in August 2014, mainly engaged in the development, production and sales of ionic liquids, ribose, nucleosides, nucleotides and related chemicals; Products are mainly used in new energy, new ma
Appearance:95%+ Package:R&D,Pilot run Transportation:per client require Port:Express ,Air, Sea
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
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Negotiable
Type:Lab/Research institutions
inquiry13-[(2'R,4'S,5'R)-3'-t-butoxycarbonyl-2'-(1'''-naphthyl)-4'-phenyl-1,3-oxazolidine-5-carbonyl]-7,10-(di-2'',2'',2''-trichloroethoxy carbonyl)-10-deacetylbaccatin III
7,10-bis-O-(2,2,2-trichloroethoxycarbonyl)docetaxel
Conditions | Yield |
---|---|
Stage #1: 13-[(2'R,4'S,5'R)-3'-t-butoxycarbonyl-2'-(1'''-naphthyl)-4'-phenyl-1,3-oxazolidine-5-carbonyl]-7,10-(di-2'',2'',2''-trichloroethoxy carbonyl)-10-deacetylbaccatin III With toluene-4-sulfonic acid In chloroform at 20℃; for 3h; Stage #2: With water; sodium hydrogencarbonate In chloroform | 88% |
With methanol; toluene-4-sulfonic acid In chloroform at 20℃; for 3h; | 88% |
di-tert-butyl dicarbonate
10-deacetyl-7,10-diTroc-baccatin III
7,10-bis-O-(2,2,2-trichloroethoxycarbonyl)docetaxel
Conditions | Yield |
---|---|
With sodium hydrogencarbonate In tetrahydrofuran at 20℃; | 87% |
In water; ethyl acetate at 25 - 30℃; for 1h; | |
With sodium hydrogencarbonate In water at 55 - 65℃; for 2h; | 737.4 g |
di-tert-butyl dicarbonate
C44H45Cl6N3O16
7,10-bis-O-(2,2,2-trichloroethoxycarbonyl)docetaxel
Conditions | Yield |
---|---|
With potassium hydrogencarbonate; triphenylphosphine In dichloromethane; water for 19h; Ambient temperature; | 63% |
N-chloro-N-sodio-tert-butylcarbamate
A
7,10-bis-O-(2,2,2-trichloroethoxycarbonyl)docetaxel
B
C49H55Cl6NO18
C
C49H55Cl6NO18
D
C49H55Cl6NO18
Conditions | Yield |
---|---|
With osmium(VIII) oxide; silver nitrate In acetonitrile; tert-butyl alcohol for 24h; Ambient temperature; var. solvents and temp.; Further byproducts given; | A 25% B 22% C 21.5% D 16.5% |
C57H61Cl6NO19
7,10-bis-O-(2,2,2-trichloroethoxycarbonyl)docetaxel
Conditions | Yield |
---|---|
With APTS In methanol at 20℃; for 16h; | 25% |
With toluene-4-sulfonic acid In methanol at 20℃; | |
With hydrogenchloride In water; ethyl acetate at 20 - 24℃; Solvent; Temperature; |
N-chloro-N-sodio-tert-butylcarbamate
C44H46Cl6O17
B
7,10-bis-O-(2,2,2-trichloroethoxycarbonyl)docetaxel
C
C49H55Cl6NO18
D
C49H55Cl6NO18
Conditions | Yield |
---|---|
With osmium(VIII) oxide; silver nitrate In toluene; tert-butyl alcohol at 4℃; for 24h; var. solvents and temp.; Further byproducts given; | A 12% B 20% C 17% D 18% |
methyl (2S,3R)-3-phenyl-2,3-dihydroxypropanoate
7,10-bis-O-(2,2,2-trichloroethoxycarbonyl)docetaxel
Conditions | Yield |
---|---|
Multi-step reaction with 6 steps 1: triethylamine / CH2Cl2 / 38 h / 0 °C 2: K2CO3 / dimethylformamide; H2O / 24 h / Ambient temperature 3: 80 percent / LiOH*H2O / methanol; H2O / 1 h / Ambient temperature 4: 91 percent / dicyclohexylcarbodiimide, 4-N,N-dimethylaminopyridine / toluene / 1 h / 80 °C 5: 78 percent / sodium azide, methyl formate / methanol; H2O / 40 h / 50 °C / other reagent: tri-n-butyltinazide/ZnI2 6: 63 percent / KHCO3, PPh3 / CH2Cl2; H2O / 19 h / Ambient temperature View Scheme |
(2S,3R)-(-)-methyl 3-hydroxy-3-phenyl-2-((p-tolylsulfonyl)oxy)propionate
7,10-bis-O-(2,2,2-trichloroethoxycarbonyl)docetaxel
Conditions | Yield |
---|---|
Multi-step reaction with 5 steps 1: K2CO3 / dimethylformamide; H2O / 24 h / Ambient temperature 2: 80 percent / LiOH*H2O / methanol; H2O / 1 h / Ambient temperature 3: 91 percent / dicyclohexylcarbodiimide, 4-N,N-dimethylaminopyridine / toluene / 1 h / 80 °C 4: 78 percent / sodium azide, methyl formate / methanol; H2O / 40 h / 50 °C / other reagent: tri-n-butyltinazide/ZnI2 5: 63 percent / KHCO3, PPh3 / CH2Cl2; H2O / 19 h / Ambient temperature View Scheme |
(2R,3R)-(+)-methyl 3-phenyloxiranecarboxylate
7,10-bis-O-(2,2,2-trichloroethoxycarbonyl)docetaxel
Conditions | Yield |
---|---|
Multi-step reaction with 4 steps 1: 80 percent / LiOH*H2O / methanol; H2O / 1 h / Ambient temperature 2: 91 percent / dicyclohexylcarbodiimide, 4-N,N-dimethylaminopyridine / toluene / 1 h / 80 °C 3: 78 percent / sodium azide, methyl formate / methanol; H2O / 40 h / 50 °C / other reagent: tri-n-butyltinazide/ZnI2 4: 63 percent / KHCO3, PPh3 / CH2Cl2; H2O / 19 h / Ambient temperature View Scheme |
methyl (2R,3S)-3-phenylglycidate
7,10-bis-O-(2,2,2-trichloroethoxycarbonyl)docetaxel
Conditions | Yield |
---|---|
Multi-step reaction with 5 steps 1: NaOH / tetrahydrofuran; H2O / 0.33 h / Ambient temperature 2: 5.55 g / dicyclohexylcarbodiimide, 4-N,N-dimethylaminopyridine / toluene / 0.17 h / Ambient temperature 3: 76 percent / hexamethylphosphoramide, TiBr4 / CH2Cl2 / 18 h / 0 °C 4: 71 percent / sodium azide, 15-crown-5 / dimethylformamide / 18 h / 0 °C 5: 63 percent / KHCO3, PPh3 / CH2Cl2; H2O / 19 h / Ambient temperature View Scheme |
Methyl cinnamate
7,10-bis-O-(2,2,2-trichloroethoxycarbonyl)docetaxel
Conditions | Yield |
---|---|
Multi-step reaction with 7 steps 1: 65 percent / AD-mix-β / 2-methyl-propan-2-ol; H2O / 18 h / Ambient temperature 2: triethylamine / CH2Cl2 / 38 h / 0 °C 3: K2CO3 / dimethylformamide; H2O / 24 h / Ambient temperature 4: 80 percent / LiOH*H2O / methanol; H2O / 1 h / Ambient temperature 5: 91 percent / dicyclohexylcarbodiimide, 4-N,N-dimethylaminopyridine / toluene / 1 h / 80 °C 6: 78 percent / sodium azide, methyl formate / methanol; H2O / 40 h / 50 °C / other reagent: tri-n-butyltinazide/ZnI2 7: 63 percent / KHCO3, PPh3 / CH2Cl2; H2O / 19 h / Ambient temperature View Scheme |
cis-2,3-epoxy-3-phenyl-1-propanoic acid
7,10-bis-O-(2,2,2-trichloroethoxycarbonyl)docetaxel
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1: 91 percent / dicyclohexylcarbodiimide, 4-N,N-dimethylaminopyridine / toluene / 1 h / 80 °C 2: 78 percent / sodium azide, methyl formate / methanol; H2O / 40 h / 50 °C / other reagent: tri-n-butyltinazide/ZnI2 3: 63 percent / KHCO3, PPh3 / CH2Cl2; H2O / 19 h / Ambient temperature View Scheme |
C44H44Cl6O16
7,10-bis-O-(2,2,2-trichloroethoxycarbonyl)docetaxel
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1: 76 percent / hexamethylphosphoramide, TiBr4 / CH2Cl2 / 18 h / 0 °C 2: 71 percent / sodium azide, 15-crown-5 / dimethylformamide / 18 h / 0 °C 3: 63 percent / KHCO3, PPh3 / CH2Cl2; H2O / 19 h / Ambient temperature View Scheme |
13-O-((2R,3R)-3-phenylglycidoyl)-7,10-O,O'-bis(2,2,2-trichloroethoxycarbonyl)-10-deacetylbaccatin
7,10-bis-O-(2,2,2-trichloroethoxycarbonyl)docetaxel
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1: 78 percent / sodium azide, methyl formate / methanol; H2O / 40 h / 50 °C / other reagent: tri-n-butyltinazide/ZnI2 2: 63 percent / KHCO3, PPh3 / CH2Cl2; H2O / 19 h / Ambient temperature View Scheme |
13-O-((2S,3R)-3-bromo-2-hydroxy-3-phenylpropionyl)-7,10-O,O'-bis(2,2,2-trichloroethoxycarbonyl)-10-deacetylbaccatin
7,10-bis-O-(2,2,2-trichloroethoxycarbonyl)docetaxel
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1: 71 percent / sodium azide, 15-crown-5 / dimethylformamide / 18 h / 0 °C 2: 63 percent / KHCO3, PPh3 / CH2Cl2; H2O / 19 h / Ambient temperature View Scheme |
(2R,3S)-3-phenyloxiranecarboxylic acid
7,10-bis-O-(2,2,2-trichloroethoxycarbonyl)docetaxel
Conditions | Yield |
---|---|
Multi-step reaction with 4 steps 1: 5.55 g / dicyclohexylcarbodiimide, 4-N,N-dimethylaminopyridine / toluene / 0.17 h / Ambient temperature 2: 76 percent / hexamethylphosphoramide, TiBr4 / CH2Cl2 / 18 h / 0 °C 3: 71 percent / sodium azide, 15-crown-5 / dimethylformamide / 18 h / 0 °C 4: 63 percent / KHCO3, PPh3 / CH2Cl2; H2O / 19 h / Ambient temperature View Scheme |
(2R,3S)-3-amino-2-hydroxy-3-phenylpropionic acid ethyl ester
7,10-bis-O-(2,2,2-trichloroethoxycarbonyl)docetaxel
Conditions | Yield |
---|---|
Multi-step reaction with 6 steps 1: 76 percent / NaHCO3 / CH2Cl2 / 20 °C 2: 99 percent / pyridinium paratoluenesulfonate (PTSP) / toluene / 80 °C 3: 100 percent / LiOH, H2O / ethanol / 20 °C 4: 98 percent / DCC, DMAP / toluene / 2 h / 80 °C 5: 78 percent / HCOOH / 4 h / 20 °C 6: 87 percent / NaHCO3 / tetrahydrofuran / 20 °C View Scheme |
(2R,3S)-3-azido-2-hydroxy-benzenepropanoic acid ethyl ester
7,10-bis-O-(2,2,2-trichloroethoxycarbonyl)docetaxel
Conditions | Yield |
---|---|
Multi-step reaction with 7 steps 1: 86 percent / H2 / 10percent Pd/C / ethyl acetate / 760 Torr 2: 76 percent / NaHCO3 / CH2Cl2 / 20 °C 3: 99 percent / pyridinium paratoluenesulfonate (PTSP) / toluene / 80 °C 4: 100 percent / LiOH, H2O / ethanol / 20 °C 5: 98 percent / DCC, DMAP / toluene / 2 h / 80 °C 6: 78 percent / HCOOH / 4 h / 20 °C 7: 87 percent / NaHCO3 / tetrahydrofuran / 20 °C View Scheme |
benzaldehyde
7,10-bis-O-(2,2,2-trichloroethoxycarbonyl)docetaxel
Conditions | Yield |
---|---|
Multi-step reaction with 10 steps 1: 1.) Et3N, Bu2BOTf / 1.) CH2Cl2, -70 to 20 deg C, 2 h, 2.) -78 to 0 deg C, 1 h 2: 81 percent / tetrahydrofuran / 0.25 h / -75 - 15 °C 3: 99 percent / NaN3, NH4Cl / ethanol / 8 h / 60 °C 4: 86 percent / H2 / 10percent Pd/C / ethyl acetate / 760 Torr 5: 76 percent / NaHCO3 / CH2Cl2 / 20 °C 6: 99 percent / pyridinium paratoluenesulfonate (PTSP) / toluene / 80 °C 7: 100 percent / LiOH, H2O / ethanol / 20 °C 8: 98 percent / DCC, DMAP / toluene / 2 h / 80 °C 9: 78 percent / HCOOH / 4 h / 20 °C 10: 87 percent / NaHCO3 / tetrahydrofuran / 20 °C View Scheme |
7,10-di-(2,2,2-trichloroethyloxycarbonyl)-10-deacetylbaccatin III
7,10-bis-O-(2,2,2-trichloroethoxycarbonyl)docetaxel
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1: 98 percent / DCC, DMAP / toluene / 2 h / 80 °C 2: 78 percent / HCOOH / 4 h / 20 °C 3: 87 percent / NaHCO3 / tetrahydrofuran / 20 °C View Scheme | |
Multi-step reaction with 2 steps 1: dmap; dicyclohexyl-carbodiimide / toluene / 50 °C 2: sodium carbonate; dihydrogen peroxide / water; tetrahydrofuran / 20 °C View Scheme | |
Multi-step reaction with 3 steps 1: dmap; dicyclohexyl-carbodiimide / toluene / 50 °C 2: sodium carbonate; dihydrogen peroxide / water; tetrahydrofuran / 20 °C 3: triphenylphosphine; diethylazodicarboxylate; 4-nitro-benzoic acid / tetrahydrofuran View Scheme |
ethyl (2R,3R)-3-phenyl-2,3-oxiranepropanoate
7,10-bis-O-(2,2,2-trichloroethoxycarbonyl)docetaxel
Conditions | Yield |
---|---|
Multi-step reaction with 8 steps 1: 99 percent / NaN3, NH4Cl / ethanol / 8 h / 60 °C 2: 86 percent / H2 / 10percent Pd/C / ethyl acetate / 760 Torr 3: 76 percent / NaHCO3 / CH2Cl2 / 20 °C 4: 99 percent / pyridinium paratoluenesulfonate (PTSP) / toluene / 80 °C 5: 100 percent / LiOH, H2O / ethanol / 20 °C 6: 98 percent / DCC, DMAP / toluene / 2 h / 80 °C 7: 78 percent / HCOOH / 4 h / 20 °C 8: 87 percent / NaHCO3 / tetrahydrofuran / 20 °C View Scheme |
(2R,3S) ethyl N-(t-butoxycarbonyl)-3-phenylisoserine
7,10-bis-O-(2,2,2-trichloroethoxycarbonyl)docetaxel
Conditions | Yield |
---|---|
Multi-step reaction with 5 steps 1: 99 percent / pyridinium paratoluenesulfonate (PTSP) / toluene / 80 °C 2: 100 percent / LiOH, H2O / ethanol / 20 °C 3: 98 percent / DCC, DMAP / toluene / 2 h / 80 °C 4: 78 percent / HCOOH / 4 h / 20 °C 5: 87 percent / NaHCO3 / tetrahydrofuran / 20 °C View Scheme |
(4S,5R)-3-(tert-butoxycarbonyl)-2,2-dimethyl-4-phenyloxazolidine-5-carboxylic acid
7,10-bis-O-(2,2,2-trichloroethoxycarbonyl)docetaxel
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1: 98 percent / DCC, DMAP / toluene / 2 h / 80 °C 2: 78 percent / HCOOH / 4 h / 20 °C 3: 87 percent / NaHCO3 / tetrahydrofuran / 20 °C View Scheme |
ethyl (4S,5R)-3-tert-butoxycarbonyl-2,2-dimethyl-4-phenyl-5-oxazolidinecarboxylate
7,10-bis-O-(2,2,2-trichloroethoxycarbonyl)docetaxel
Conditions | Yield |
---|---|
Multi-step reaction with 4 steps 1: 100 percent / LiOH, H2O / ethanol / 20 °C 2: 98 percent / DCC, DMAP / toluene / 2 h / 80 °C 3: 78 percent / HCOOH / 4 h / 20 °C 4: 87 percent / NaHCO3 / tetrahydrofuran / 20 °C View Scheme |
(4S,5R)-3-((2S,3R)-2-Bromo-3-hydroxy-3-phenyl-propionyl)-4-methyl-5-phenyl-oxazolidin-2-one
7,10-bis-O-(2,2,2-trichloroethoxycarbonyl)docetaxel
Conditions | Yield |
---|---|
Multi-step reaction with 9 steps 1: 81 percent / tetrahydrofuran / 0.25 h / -75 - 15 °C 2: 99 percent / NaN3, NH4Cl / ethanol / 8 h / 60 °C 3: 86 percent / H2 / 10percent Pd/C / ethyl acetate / 760 Torr 4: 76 percent / NaHCO3 / CH2Cl2 / 20 °C 5: 99 percent / pyridinium paratoluenesulfonate (PTSP) / toluene / 80 °C 6: 100 percent / LiOH, H2O / ethanol / 20 °C 7: 98 percent / DCC, DMAP / toluene / 2 h / 80 °C 8: 78 percent / HCOOH / 4 h / 20 °C 9: 87 percent / NaHCO3 / tetrahydrofuran / 20 °C View Scheme |
4-acetoxy-2α-benzoyloxy-5β,20-epoxy-1-hydroxy-9-oxo-7β,10β-bis[(2,2,2-tri-chloroethoxy)carbonyloxy]-11-taxen-13α-yl (4S,5R)-3-tert-butoxycarbonyl-2,2-dimethyl-4-phenyl-5-oxazolidinecarboxylate
7,10-bis-O-(2,2,2-trichloroethoxycarbonyl)docetaxel
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1: 78 percent / HCOOH / 4 h / 20 °C 2: 87 percent / NaHCO3 / tetrahydrofuran / 20 °C View Scheme | |
Multi-step reaction with 2 steps 1: formic acid / 1 h / 25 - 35 °C 2: sodium hydrogencarbonate / water / 2 h / 55 - 65 °C View Scheme |
A
(2'R,3'S)-7,10-di-Troc-docetaxel
B
7,10-bis-O-(2,2,2-trichloroethoxycarbonyl)docetaxel
Conditions | Yield |
---|---|
With silica gel column (20 μM, 0.45*90 cm) In methanol; dichloromethane Purification / work up; Resolution of diastereomeric mixture; |
(2'R,3'S)-7,10-di-Troc-docetaxel
7,10-bis-O-(2,2,2-trichloroethoxycarbonyl)docetaxel
Conditions | Yield |
---|---|
Stage #1: (2'R,3'S)-7,10-di-Troc-docetaxel With triphenylphosphine; diethylazodicarboxylate; 4-nitro-benzoic acid In tetrahydrofuran Stage #2: With potassium hydroxide In tetrahydrofuran | |
Stage #1: (2'R,3'S)-7,10-di-Troc-docetaxel With triphenylphosphine; diethylazodicarboxylate; 4-nitro-benzoic acid In tetrahydrofuran Stage #2: With potassium hydroxide In tetrahydrofuran |
7,10-bis-O-(2,2,2-trichloroethoxycarbonyl)docetaxel
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1: sodium carbonate; dihydrogen peroxide / water; tetrahydrofuran / 20 °C 2: triphenylphosphine; diethylazodicarboxylate; 4-nitro-benzoic acid / tetrahydrofuran View Scheme |
A
(2'R,3'S)-7,10-di-Troc-docetaxel
B
7,10-bis-O-(2,2,2-trichloroethoxycarbonyl)docetaxel
Conditions | Yield |
---|---|
With dihydrogen peroxide; sodium carbonate In tetrahydrofuran; water at 20℃; |
7,10-bis-O-(2,2,2-trichloroethoxycarbonyl)docetaxel
N,N'-dimethyl-N-benzyl-[4-(2,3,4-tri-O-tert-butyldimethylsilyl-β-D-glucopyranosyl)uronate-3-nitrobenzoyloxycarbonyl]ethylenediamine carbamoyl chloride
Conditions | Yield |
---|---|
With dmap In dichloromethane for 2h; | 93% |
7,10-bis-O-(2,2,2-trichloroethoxycarbonyl)docetaxel
Conditions | Yield |
---|---|
With acetic acid; zinc In methanol at 60℃; for 2h; | 90% |
With acetic acid; zinc In methanol at 60℃; for 1h; | 90% |
Product distribution / selectivity; | 90% |
7,10-bis-O-(2,2,2-trichloroethoxycarbonyl)docetaxel
10-deacetyl-7,10-diTroc-baccatin III
Conditions | Yield |
---|---|
With trimethylsilyl iodide In acetonitrile at 0℃; for 0.5h; | 75% |
With formic acid at 18℃; for 1.5h; Temperature; | 25.3 g |
glutaric anhydride,
7,10-bis-O-(2,2,2-trichloroethoxycarbonyl)docetaxel
Conditions | Yield |
---|---|
With pyridine at -20 - 25℃; | 60% |
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