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Chemvon Biotechnology Co. Ltd.

Chemvon Biotechnology is one of the leading high-technology manufacturer in the field of pharmaceutical and fine chemical industry. From origins as a research group in technology service, chemvon has progressed into an integrated company with a k

Dorzolamide

Cas:120279-96-1

Min.Order:0 Metric Ton

Negotiable

Type:Lab/Research institutions

inquiry

Dayang Chem (Hangzhou) Co.,Ltd.

As 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

Dorzolamide Manufacturer/High quality/Best price/In stock

Cas:120279-96-1

Min.Order:1 Kilogram

FOB Price: $3.0

Type:Lab/Research institutions

inquiry

Henan Tianfu Chemical Co., Ltd.

Our company engages in Sodium Tripolyphosphate (STPP) and Sodium Hexametabphosphate (SHMP) production; development of noble metal catalysts, synthesis of electronic chemical materials and general chemicals Imp&Exp trading business. The company

TIANFU-CHEM - Dorzolamide

Cas:120279-96-1

Min.Order:1 Kilogram

FOB Price: $1000.0

Type:Lab/Research institutions

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Hebei Nengqian Chemical Import and Export Co., LTD

Our Advantage Rich Experience Our products are sold all over Europe,North&South America, Sino-East, Asia and pacific area as well as Africa,we establish long term. Quality service Company cooperates with research institutes. We strictly con

Dorzolamide CAS 120279-96-1

Cas:120279-96-1

Min.Order:1 Kilogram

FOB Price: $1.0 / 10.0

Type:Trading Company

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Zhuozhou Wenxi import and Export Co., Ltd

WITH 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

Hot product CAS 120279-96-1 with high-quality service

Cas:120279-96-1

Min.Order:10 Gram

FOB Price: $146.0 / 176.0

Type:Trading Company

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Henan Sinotech Import&Export Corporation

[English Name] Dorzolamide [CAS No.] 120279-96-1 [Mol. Formula ] C10H16N2O4S3 Appearance:White powder Storage:Store in cool and dry place, away from sun light. Package:drum Application:Eye Treatment Drug; Miotic, Antiglaucoma Transportation:B

Dorzolamide

Cas:120279-96-1

Min.Order:1 Kilogram

FOB Price: $1.0

Type:Other

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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

Dorzolamide 120279-96-1

Cas:120279-96-1

Min.Order:1 Kilogram

Negotiable

Type:Lab/Research institutions

inquiry

Qingdao Beluga Import and Export Co., LTD

Dorzolamide CAS:120279-96-1 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 intermediate

Dorzolamide CAS:120279-96-1

Cas:120279-96-1

Min.Order:1 Gram

Negotiable

Type:Lab/Research institutions

inquiry

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

Dorzolamide

Cas:120279-96-1

Min.Order:1 Kilogram

Negotiable

Type:Lab/Research institutions

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Changchun Artel lmport and Export trade company

Superiority We can customize and synthesize products that other suppliers may not be able to provide. Advantage cof, mof ligand manufacturer best service, company and transport

99% Dorzolamide CAS:120279-96-1

Cas:120279-96-1

Min.Order:100 Kilogram

Negotiable

Type:Trading Company

inquiry

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

Dorzolamide

Cas:120279-96-1

Min.Order:0

Negotiable

Type:Lab/Research institutions

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Afine Chemicals Limited

Our Services 1. New Molecules R&D 2. Own test center HPLC NMR GC LC-MS 3. API and Intermediates from China reputed manufacturers 4. Documents support COA MOA MSDS DMF open part Our advantages 1. Government awarded company. Top 100 enter

Dorzolamide

Cas:120279-96-1

Min.Order:1 Kilogram

FOB Price: $1.0 / 100000.0

Type:Lab/Research institutions

inquiry

Hangzhou Keyingchem Co.,Ltd

Hangzhou KeyingChem Co., Ltd. exported this product to many countries and regions at best price. If you are looking for the material’s manufacturer or supplier in China, KeyingChem is your best choice. Pls contact with us freely for getting det

Dorzolamide

Cas:120279-96-1

Min.Order:0 Metric Ton

Negotiable

Type:Lab/Research institutions

inquiry

Hangzhou J&H Chemical Co., Ltd.

J&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

Dorzolamide

Cas:120279-96-1

Min.Order:0

Negotiable

Type:Lab/Research institutions

inquiry

Chemlyte Solutions

Chemlyte Solutions believe that customers and suppliers deserve much more than what traditional distributors can offer. To grow in today s fast-paced and increasingly competitive market it is essential to be able to quickly adapt to market forces eff

Featured products Dorzolamide

Cas:120279-96-1

Min.Order:100 Gram

Negotiable

Type:Other

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

Dorzolamide

Cas:120279-96-1

Min.Order:10 Gram

FOB Price: $100.0

Type:Lab/Research institutions

inquiry

Ality Chemical Corporation

The 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

Factory Supply Dorzolamide

Cas:120279-96-1

Min.Order:0

Negotiable

Type:Other

inquiry

Zibo Dorne chemical technology co. LTD

Product 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,

Dorzolamide

Cas:120279-96-1

Min.Order:1 Gram

Negotiable

Type:Lab/Research institutions

inquiry

Jiangsu Qianyu Molecular Technology Co., LTD.

Our Advantages A. International Top level TechnologyOur company owned biomedicine experts are famous at home and abroad with rich experience in research and development in the field of efficient chiral functional molecules research and development an

Top Purity Dorzolamide

Cas:120279-96-1

Min.Order:0

Negotiable

Type:Trading Company

inquiry

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,

Dorzolamide

Cas:120279-96-1

Min.Order:1 Milligram

Negotiable

Type:Trading Company

inquiry

Hangzhou Think Chemical Co. Ltd

HANGZHOU THINK CHEMICAL CO., LTD. (THINKCHEM) is an integrative corporation of trade, research and contract manufacture. With about ten years of business experiences on the marketing & distribution, thinkchem specializes in exp

Dorzolamide HCl CAS:120279-96-1

Cas:120279-96-1

Min.Order:0 Metric Ton

Negotiable

Type:Other

inquiry

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

Dorzolamide

Cas:120279-96-1

Min.Order:1 Kilogram

FOB Price: $18.0 / 20.0

Type:Trading Company

inquiry

TAIZHOU ZHENYU BIOTECHNOLOGY CO., LTD

Zhenyu biotech exported this product to many countries and regions at best price. if you are looking for the material's manufacturer or supplier in china, zhenyu biotech is your best choice. pls contact with us freely for getting detailed

Dorzolamide

Cas:120279-96-1

Min.Order:1 Kilogram

FOB Price: $2.0

Type:Lab/Research institutions

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

Dorzolamide

Cas:120279-96-1

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

99% Dorzolamide CAS:120279-96-1 CAS NO.120279-96-1

Cas:120279-96-1

Min.Order:1 Metric Ton

FOB Price: $7.0 / 8.0

Type:Trading Company

inquiry

Hunan chemfish Pharmaceutical co.,Ltd

Appearance:95%+ Package:R&D,Pilot run Transportation:per client require Port:Express ,Air, Sea

Dorzolamide

Cas:120279-96-1

Min.Order:0

Negotiable

Type:Manufacturers

inquiry

Suzhou Health Chemicals Co., Ltd.

High quality,stable supply chain.Appearance:white/off-white or light yellow Storage:Store in cool and dry place, keep away from strong light and heat. Package:aluminum bottle,glass bottle,PTFE bottle,cardboard drum Application:Active Pharmaceutical I

Dorzolamide

Cas:120279-96-1

Min.Order:0

Negotiable

Type:Lab/Research institutions

inquiry

Golden Pharma Co., Limited

GOLDEN PHARMA CO.,LIMITED.is a professional pharmaceutical company,our team have more than 20years expereince in pharmaceutical production and sales. we are a professional technical enterprise specializing in the R & D, production,QA regulation

Dorzolamide

Cas:120279-96-1

Min.Order:1 Kilogram

Negotiable

Type:Other

inquiry

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

Dorzolamide

Cas:120279-96-1

Min.Order:1 Metric Ton

FOB Price: $1.0

Type:Trading Company

inquiry

Kono Chem Co.,Ltd

high purity lowest priceAppearance:solid or liquid Storage:in sealed air resistant place Package:drum and bag Application:for pharma use Transportation:by sea or air Port:Beijing or Guangzhou

Dorzolamide

Cas:120279-96-1

Min.Order:0

Negotiable

Type:Other

inquiry

Synthetic route

(4S,6S)‑4‑acetamido‑5,6‑dihydro‑6‑methyl‑4H‑thieno[2,3‑b]thiopyran‑2‑sulfonamide‑7,7‑dioxide
147200-03-1

(4S,6S)‑4‑acetamido‑5,6‑dihydro‑6‑methyl‑4H‑thieno[2,3‑b]thiopyran‑2‑sulfonamide‑7,7‑dioxide

dorzolamide
120279-96-1

dorzolamide

Conditions
ConditionsYield
With zinc(II) tetrahydroborate In methanol at 90℃; for 3h; Temperature; Solvent; Green chemistry;90%
N-ethyl-N-[(4S,6S)-6-methyl-7,7-dioxo-2-sulfamoyl-4,5,6,7-tetrahydro-7λ6-thieno[2,3-b]thiopyran-4-yl]acetamide

N-ethyl-N-[(4S,6S)-6-methyl-7,7-dioxo-2-sulfamoyl-4,5,6,7-tetrahydro-7λ6-thieno[2,3-b]thiopyran-4-yl]acetamide

dorzolamide
120279-96-1

dorzolamide

Conditions
ConditionsYield
With hydrogenchloride; water In methanol for 72h; Heating / reflux;66%
4-(acetylamino)-5,6-dihydro-(S)-6-methyl-4H-thieno<2,3-b>thiopyran-2-sulfonamide 7,7-dioxide

4-(acetylamino)-5,6-dihydro-(S)-6-methyl-4H-thieno<2,3-b>thiopyran-2-sulfonamide 7,7-dioxide

dorzolamide
120279-96-1

dorzolamide

Conditions
ConditionsYield
With dimethylsulfide borane complex; sulfuric acid 1) THF, r.t.; Yield given. Multistep reaction;
(S)-5,6-dihydro-6-methylthieno<2,3-b>thiopyran-4-one
147086-79-1

(S)-5,6-dihydro-6-methylthieno<2,3-b>thiopyran-4-one

dorzolamide
120279-96-1

dorzolamide

Conditions
ConditionsYield
Multi-step reaction with 7 steps
1: LiAlH4 / tetrahydrofuran; toluene / 0 - 5 °C
2: 24 g / sodium tungstate dihydrate, 30 percent hydrogen peroxide / H2O; ethyl acetate; toluene / 1) 0 - 15 deg C, 30 min, 2) 25 deg C, 2 h
3: 95 percent / pyridine / tetrahydrofuran / 48 h / 25 - 30 °C
4: 89.6 percent / H2SO4 / 20 - 25 °C
5: chlorosulfonic acid / 12 h / 50 °C
6: conc. NH4OH / tetrahydrofuran / 1 h / 0 - 5 °C
7: 1) borane-dimethyl sulfide, 2) H2SO4 / 1) THF, r.t.
View Scheme
Multi-step reaction with 7 steps
1: LiAlH4 / tetrahydrofuran; toluene / 0 - 5 °C
2: 24 g / sodium tungstate dihydrate, 30 percent hydrogen peroxide / H2O; ethyl acetate; toluene / 1) 0 - 15 deg C, 30 min, 2) 25 deg C, 2 h
3: H2SO4 / -5 °C
4: H2SO4 / -5 °C
5: chlorosulfonic acid / 12 h / 50 °C
6: conc. NH4OH / tetrahydrofuran / 1 h / 0 - 5 °C
7: 1) borane-dimethyl sulfide, 2) H2SO4 / 1) THF, r.t.
View Scheme
Multi-step reaction with 6 steps
1: LiAlH4 / tetrahydrofuran; toluene / 0 - 5 °C
2: 24 g / sodium tungstate dihydrate, 30 percent hydrogen peroxide / H2O; ethyl acetate; toluene / 1) 0 - 15 deg C, 30 min, 2) 25 deg C, 2 h
3: 1) conc. H2SO4 / 1) THF, 48 h, r.t., 2) overnight
4: chlorosulfonic acid / 12 h / 50 °C
5: conc. NH4OH / tetrahydrofuran / 1 h / 0 - 5 °C
6: 1) borane-dimethyl sulfide, 2) H2SO4 / 1) THF, r.t.
View Scheme
5,6-dihydro-(R)-4-hydroxy-(S)-6-methyl-4H-thieno<2,3-b>thiopyran
147086-80-4

5,6-dihydro-(R)-4-hydroxy-(S)-6-methyl-4H-thieno<2,3-b>thiopyran

dorzolamide
120279-96-1

dorzolamide

Conditions
ConditionsYield
Multi-step reaction with 6 steps
1: 24 g / sodium tungstate dihydrate, 30 percent hydrogen peroxide / H2O; ethyl acetate; toluene / 1) 0 - 15 deg C, 30 min, 2) 25 deg C, 2 h
2: 95 percent / pyridine / tetrahydrofuran / 48 h / 25 - 30 °C
3: 89.6 percent / H2SO4 / 20 - 25 °C
4: chlorosulfonic acid / 12 h / 50 °C
5: conc. NH4OH / tetrahydrofuran / 1 h / 0 - 5 °C
6: 1) borane-dimethyl sulfide, 2) H2SO4 / 1) THF, r.t.
View Scheme
Multi-step reaction with 6 steps
1: 24 g / sodium tungstate dihydrate, 30 percent hydrogen peroxide / H2O; ethyl acetate; toluene / 1) 0 - 15 deg C, 30 min, 2) 25 deg C, 2 h
2: H2SO4 / -5 °C
3: H2SO4 / -5 °C
4: chlorosulfonic acid / 12 h / 50 °C
5: conc. NH4OH / tetrahydrofuran / 1 h / 0 - 5 °C
6: 1) borane-dimethyl sulfide, 2) H2SO4 / 1) THF, r.t.
View Scheme
Multi-step reaction with 5 steps
1: 24 g / sodium tungstate dihydrate, 30 percent hydrogen peroxide / H2O; ethyl acetate; toluene / 1) 0 - 15 deg C, 30 min, 2) 25 deg C, 2 h
2: 1) conc. H2SO4 / 1) THF, 48 h, r.t., 2) overnight
3: chlorosulfonic acid / 12 h / 50 °C
4: conc. NH4OH / tetrahydrofuran / 1 h / 0 - 5 °C
5: 1) borane-dimethyl sulfide, 2) H2SO4 / 1) THF, r.t.
View Scheme
(S)-3-(thien-2-ylthio)butyric acid
133359-80-5

(S)-3-(thien-2-ylthio)butyric acid

dorzolamide
120279-96-1

dorzolamide

Conditions
ConditionsYield
Multi-step reaction with 8 steps
1: trifluoroacetic anhydride / toluene / 1 h / 25 °C
2: LiAlH4 / tetrahydrofuran; toluene / 0 - 5 °C
3: 24 g / sodium tungstate dihydrate, 30 percent hydrogen peroxide / H2O; ethyl acetate; toluene / 1) 0 - 15 deg C, 30 min, 2) 25 deg C, 2 h
4: 95 percent / pyridine / tetrahydrofuran / 48 h / 25 - 30 °C
5: 89.6 percent / H2SO4 / 20 - 25 °C
6: chlorosulfonic acid / 12 h / 50 °C
7: conc. NH4OH / tetrahydrofuran / 1 h / 0 - 5 °C
8: 1) borane-dimethyl sulfide, 2) H2SO4 / 1) THF, r.t.
View Scheme
Multi-step reaction with 8 steps
1: trifluoroacetic anhydride / toluene / 1 h / 25 °C
2: LiAlH4 / tetrahydrofuran; toluene / 0 - 5 °C
3: 24 g / sodium tungstate dihydrate, 30 percent hydrogen peroxide / H2O; ethyl acetate; toluene / 1) 0 - 15 deg C, 30 min, 2) 25 deg C, 2 h
4: H2SO4 / -5 °C
5: H2SO4 / -5 °C
6: chlorosulfonic acid / 12 h / 50 °C
7: conc. NH4OH / tetrahydrofuran / 1 h / 0 - 5 °C
8: 1) borane-dimethyl sulfide, 2) H2SO4 / 1) THF, r.t.
View Scheme
Multi-step reaction with 7 steps
1: trifluoroacetic anhydride / toluene / 1 h / 25 °C
2: LiAlH4 / tetrahydrofuran; toluene / 0 - 5 °C
3: 24 g / sodium tungstate dihydrate, 30 percent hydrogen peroxide / H2O; ethyl acetate; toluene / 1) 0 - 15 deg C, 30 min, 2) 25 deg C, 2 h
4: 1) conc. H2SO4 / 1) THF, 48 h, r.t., 2) overnight
5: chlorosulfonic acid / 12 h / 50 °C
6: conc. NH4OH / tetrahydrofuran / 1 h / 0 - 5 °C
7: 1) borane-dimethyl sulfide, 2) H2SO4 / 1) THF, r.t.
View Scheme
(S)-6-Methyl-6H-thieno[2,3-b]thiopyran 7,7-dioxide
147086-84-8

(S)-6-Methyl-6H-thieno[2,3-b]thiopyran 7,7-dioxide

dorzolamide
120279-96-1

dorzolamide

Conditions
ConditionsYield
Multi-step reaction with 4 steps
1: H2SO4 / -5 °C
2: chlorosulfonic acid / 12 h / 50 °C
3: conc. NH4OH / tetrahydrofuran / 1 h / 0 - 5 °C
4: 1) borane-dimethyl sulfide, 2) H2SO4 / 1) THF, r.t.
View Scheme
methyl (S)-3-(thiophen-2-ylthio)butyrate
133359-79-2

methyl (S)-3-(thiophen-2-ylthio)butyrate

dorzolamide
120279-96-1

dorzolamide

Conditions
ConditionsYield
Multi-step reaction with 9 steps
1: 45 g / 12 N HCl / H2O / 3 h / Heating
2: trifluoroacetic anhydride / toluene / 1 h / 25 °C
3: LiAlH4 / tetrahydrofuran; toluene / 0 - 5 °C
4: 24 g / sodium tungstate dihydrate, 30 percent hydrogen peroxide / H2O; ethyl acetate; toluene / 1) 0 - 15 deg C, 30 min, 2) 25 deg C, 2 h
5: 95 percent / pyridine / tetrahydrofuran / 48 h / 25 - 30 °C
6: 89.6 percent / H2SO4 / 20 - 25 °C
7: chlorosulfonic acid / 12 h / 50 °C
8: conc. NH4OH / tetrahydrofuran / 1 h / 0 - 5 °C
9: 1) borane-dimethyl sulfide, 2) H2SO4 / 1) THF, r.t.
View Scheme
Multi-step reaction with 9 steps
1: 45 g / 12 N HCl / H2O / 3 h / Heating
2: trifluoroacetic anhydride / toluene / 1 h / 25 °C
3: LiAlH4 / tetrahydrofuran; toluene / 0 - 5 °C
4: 24 g / sodium tungstate dihydrate, 30 percent hydrogen peroxide / H2O; ethyl acetate; toluene / 1) 0 - 15 deg C, 30 min, 2) 25 deg C, 2 h
5: H2SO4 / -5 °C
6: H2SO4 / -5 °C
7: chlorosulfonic acid / 12 h / 50 °C
8: conc. NH4OH / tetrahydrofuran / 1 h / 0 - 5 °C
9: 1) borane-dimethyl sulfide, 2) H2SO4 / 1) THF, r.t.
View Scheme
Multi-step reaction with 8 steps
1: 45 g / 12 N HCl / H2O / 3 h / Heating
2: trifluoroacetic anhydride / toluene / 1 h / 25 °C
3: LiAlH4 / tetrahydrofuran; toluene / 0 - 5 °C
4: 24 g / sodium tungstate dihydrate, 30 percent hydrogen peroxide / H2O; ethyl acetate; toluene / 1) 0 - 15 deg C, 30 min, 2) 25 deg C, 2 h
5: 1) conc. H2SO4 / 1) THF, 48 h, r.t., 2) overnight
6: chlorosulfonic acid / 12 h / 50 °C
7: conc. NH4OH / tetrahydrofuran / 1 h / 0 - 5 °C
8: 1) borane-dimethyl sulfide, 2) H2SO4 / 1) THF, r.t.
View Scheme
5,6-dihydro-(R,S)-4-hydroxy-(S)-6-methyl-4H-thieno<2,3-b>thiopyran 7,7-dioxide
1034290-08-8

5,6-dihydro-(R,S)-4-hydroxy-(S)-6-methyl-4H-thieno<2,3-b>thiopyran 7,7-dioxide

dorzolamide
120279-96-1

dorzolamide

Conditions
ConditionsYield
Multi-step reaction with 5 steps
1: 95 percent / pyridine / tetrahydrofuran / 48 h / 25 - 30 °C
2: 89.6 percent / H2SO4 / 20 - 25 °C
3: chlorosulfonic acid / 12 h / 50 °C
4: conc. NH4OH / tetrahydrofuran / 1 h / 0 - 5 °C
5: 1) borane-dimethyl sulfide, 2) H2SO4 / 1) THF, r.t.
View Scheme
Multi-step reaction with 5 steps
1: H2SO4 / -5 °C
2: H2SO4 / -5 °C
3: chlorosulfonic acid / 12 h / 50 °C
4: conc. NH4OH / tetrahydrofuran / 1 h / 0 - 5 °C
5: 1) borane-dimethyl sulfide, 2) H2SO4 / 1) THF, r.t.
View Scheme
Multi-step reaction with 4 steps
1: 1) conc. H2SO4 / 1) THF, 48 h, r.t., 2) overnight
2: chlorosulfonic acid / 12 h / 50 °C
3: conc. NH4OH / tetrahydrofuran / 1 h / 0 - 5 °C
4: 1) borane-dimethyl sulfide, 2) H2SO4 / 1) THF, r.t.
View Scheme
4-(acetylamino)-5,6-dihydro-(S)-6-methyl-4H-thieno<2,3-b>thiopyran-2-sulfonyl chloride 7,7-dioxide

4-(acetylamino)-5,6-dihydro-(S)-6-methyl-4H-thieno<2,3-b>thiopyran-2-sulfonyl chloride 7,7-dioxide

dorzolamide
120279-96-1

dorzolamide

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1: conc. NH4OH / tetrahydrofuran / 1 h / 0 - 5 °C
2: 1) borane-dimethyl sulfide, 2) H2SO4 / 1) THF, r.t.
View Scheme
N-(5,6-dihydro-(S)-6-methyl-4H-thieno<2,3-b>thiopyran-4-yl)acetamide 7,7-dioxide

N-(5,6-dihydro-(S)-6-methyl-4H-thieno<2,3-b>thiopyran-4-yl)acetamide 7,7-dioxide

dorzolamide
120279-96-1

dorzolamide

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1: chlorosulfonic acid / 12 h / 50 °C
2: conc. NH4OH / tetrahydrofuran / 1 h / 0 - 5 °C
3: 1) borane-dimethyl sulfide, 2) H2SO4 / 1) THF, r.t.
View Scheme
5,6-dihydro-(R,S)-4-acetoxy-(S)-6-methyl-4H-thieno<2,3-b>thiopyran 7,7-dioxide

5,6-dihydro-(R,S)-4-acetoxy-(S)-6-methyl-4H-thieno<2,3-b>thiopyran 7,7-dioxide

dorzolamide
120279-96-1

dorzolamide

Conditions
ConditionsYield
Multi-step reaction with 4 steps
1: 89.6 percent / H2SO4 / 20 - 25 °C
2: chlorosulfonic acid / 12 h / 50 °C
3: conc. NH4OH / tetrahydrofuran / 1 h / 0 - 5 °C
4: 1) borane-dimethyl sulfide, 2) H2SO4 / 1) THF, r.t.
View Scheme
dorzolamide
120279-96-1

dorzolamide

dorzolamide hydrochloride
130693-82-2

dorzolamide hydrochloride

Conditions
ConditionsYield
With hydrogenchloride In ethyl acetate pH=1;95%
With hydrogenchloride In water; dimethyl sulfoxide at 5 - 10℃; for 3h; pH=1.0;
docosahexaenoic acid
6217-54-5

docosahexaenoic acid

dorzolamide
120279-96-1

dorzolamide

(4S,6S)-4-ethylamino-6-methyl-7,7-dioxo-4,5,6,7-tetrahydro-7λ*6*-thieno[2,3-b]thiopyran-2-sulfonic acid ((4Z,7Z,10Z,13Z,16Z,19Z)-docosa-4,7,10,13,16,19-hexaenoyl)amide

(4S,6S)-4-ethylamino-6-methyl-7,7-dioxo-4,5,6,7-tetrahydro-7λ*6*-thieno[2,3-b]thiopyran-2-sulfonic acid ((4Z,7Z,10Z,13Z,16Z,19Z)-docosa-4,7,10,13,16,19-hexaenoyl)amide

Conditions
ConditionsYield
Stage #1: dorzolamide With N-ethyl-N,N-diisopropylamine In dichloromethane at 0℃; for 0.5h; Inert atmosphere;
Stage #2: docosahexaenoic acid With dmap; benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In dichloromethane at 0 - 30℃; for 1h; Inert atmosphere;
95%
N,N-dimethyl-formamide dimethyl acetal
4637-24-5

N,N-dimethyl-formamide dimethyl acetal

dorzolamide
120279-96-1

dorzolamide

(E)-N'-{[(2S,4S)-4-(ethylamino)-2-methyl-1,1-dioxo-2H,3H,4H-1λ6-thieno[2,3-b]thiopyran-6-yl]sulfonyl}-N,N-dimethylmethanimidamide

(E)-N'-{[(2S,4S)-4-(ethylamino)-2-methyl-1,1-dioxo-2H,3H,4H-1λ6-thieno[2,3-b]thiopyran-6-yl]sulfonyl}-N,N-dimethylmethanimidamide

Conditions
ConditionsYield
With trimethylamine In N,N-dimethyl-formamide at 0 - 20℃; for 16h; Inert atmosphere;95%
(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[ (2S)-2-{[ (2S)-2-{[(2S)-2-{[(2S)-2-[(tert-butyldiphenylsilyl)oxy]propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoic acid

(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[ (2S)-2-{[ (2S)-2-{[(2S)-2-{[(2S)-2-[(tert-butyldiphenylsilyl)oxy]propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoic acid

dorzolamide
120279-96-1

dorzolamide

(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1-[(1S)-1-({[(2S,4S)-4-(ethylamino)-2-methyl-1,1-dioxo-2H,3H,4H-1λ6-thieno[2,3-b]thiopyran-6-yl]sulfonyl}carbamoyl)ethoxy]-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl (2S)-2-[(tert-butyldiphenylsilyl)oxy]propanoate

(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1-[(1S)-1-({[(2S,4S)-4-(ethylamino)-2-methyl-1,1-dioxo-2H,3H,4H-1λ6-thieno[2,3-b]thiopyran-6-yl]sulfonyl}carbamoyl)ethoxy]-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl (2S)-2-[(tert-butyldiphenylsilyl)oxy]propanoate

Conditions
ConditionsYield
Stage #1: dorzolamide With N-ethyl-N,N-diisopropylamine In dichloromethane at 0℃; for 0.5h; Inert atmosphere;
Stage #2: (2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[ (2S)-2-{[ (2S)-2-{[(2S)-2-{[(2S)-2-[(tert-butyldiphenylsilyl)oxy]propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoic acid With dmap; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In dichloromethane at 0 - 30℃; for 1h;
84%
(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-[(tert butyldiphenylsilyl)oxy]propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoic acid

(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-[(tert butyldiphenylsilyl)oxy]propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoic acid

dorzolamide
120279-96-1

dorzolamide

(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1-[(1S)-1-({[(2S,4S)-4-(ethylamino)-2-methyl-1,1-dioxo-2H,3H,4H-1λ6-thieno[2,3-b]thiopyran-6-yl]sulfonyl}carbamoyl)ethoxy]-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl (2S)-2-[(tert-butyldiphenylsilyl)oxy]propanoate

(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1-[(1S)-1-({[(2S,4S)-4-(ethylamino)-2-methyl-1,1-dioxo-2H,3H,4H-1λ6-thieno[2,3-b]thiopyran-6-yl]sulfonyl}carbamoyl)ethoxy]-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl (2S)-2-[(tert-butyldiphenylsilyl)oxy]propanoate

Conditions
ConditionsYield
Stage #1: dorzolamide With N-ethyl-N,N-diisopropylamine In dichloromethane at 0℃; Inert atmosphere;
Stage #2: (2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-[(tert butyldiphenylsilyl)oxy]propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoic acid With dmap; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In dichloromethane at 0 - 30℃; for 1h;
84%
BOC-glycine
4530-20-5

BOC-glycine

dorzolamide
120279-96-1

dorzolamide

tert‐butyl N‐[({[(2S,4S)‐4‐(ethylamino)‐2‐methyl‐1,1‐dioxo‐2H,3H,4H‐1λ6‐thieno[2,3‐b]thiopyran‐6‐yl]sulfonyl}carbamoyl)methyl]carbamate

tert‐butyl N‐[({[(2S,4S)‐4‐(ethylamino)‐2‐methyl‐1,1‐dioxo‐2H,3H,4H‐1λ6‐thieno[2,3‐b]thiopyran‐6‐yl]sulfonyl}carbamoyl)methyl]carbamate

Conditions
ConditionsYield
Stage #1: dorzolamide With triethylamine In dichloromethane at 0℃; for 0.5h; Inert atmosphere;
Stage #2: BOC-glycine With dmap; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In dichloromethane at 0 - 30℃; for 1h; Inert atmosphere;
82%
dorzolamide
120279-96-1

dorzolamide

tert-butylchlorodiphenylsilane
58479-61-1

tert-butylchlorodiphenylsilane

(2S,4S)-N-(tert-butyldiphenylsilyl)-4-(ethylamino)-2-methyl-1,1-dioxo-2H,3H,4H-1λ6-thieno[2,3-b]thiopyran-6-sulfonamide

(2S,4S)-N-(tert-butyldiphenylsilyl)-4-(ethylamino)-2-methyl-1,1-dioxo-2H,3H,4H-1λ6-thieno[2,3-b]thiopyran-6-sulfonamide

Conditions
ConditionsYield
With dmap In dichloromethane at 0 - 30℃; for 2h;76%
With dmap; N-ethyl-N,N-diisopropylamine In dichloromethane at 0 - 30℃; for 3h; Inert atmosphere;49%
2‐(2‐{[4‐(tert‐butoxy)‐4‐oxobutanoyl]oxy}‐N‐methylacetamido)acetic acid

2‐(2‐{[4‐(tert‐butoxy)‐4‐oxobutanoyl]oxy}‐N‐methylacetamido)acetic acid

dorzolamide
120279-96-1

dorzolamide

1-tert-butyl 4-{[({[(2S,4S)-4-(ethylamino)-2-methyl-1,1-dioxo-2H,3H,4H-1λ6-thieno[2,3-b]thiopyran-6-yl]sulfonyl}carbamoyl)methyl](methyl)carbamoyl}methyl butanedioate

1-tert-butyl 4-{[({[(2S,4S)-4-(ethylamino)-2-methyl-1,1-dioxo-2H,3H,4H-1λ6-thieno[2,3-b]thiopyran-6-yl]sulfonyl}carbamoyl)methyl](methyl)carbamoyl}methyl butanedioate

Conditions
ConditionsYield
With dmap; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; N-ethyl-N,N-diisopropylamine In dichloromethane at 0 - 30℃; for 4h; Inert atmosphere;74%
{[(acetyloxy)acetyl](methyl)amino}acetic acid

{[(acetyloxy)acetyl](methyl)amino}acetic acid

dorzolamide
120279-96-1

dorzolamide

{[({[(2S,4S)-4-(ethylamino)-2-methyl-1,1-dioxo-2H,3H,4H-1λ6-thieno[2,3-b]thiopyran-6-yl]sulfonyl}carbamoyl)methy](methyl)carbamoyl}methyl acetate

{[({[(2S,4S)-4-(ethylamino)-2-methyl-1,1-dioxo-2H,3H,4H-1λ6-thieno[2,3-b]thiopyran-6-yl]sulfonyl}carbamoyl)methy](methyl)carbamoyl}methyl acetate

Conditions
ConditionsYield
Stage #1: dorzolamide With triethylamine In dichloromethane at 0℃; for 0.5h; Inert atmosphere;
Stage #2: {[(acetyloxy)acetyl](methyl)amino}acetic acid With dmap; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In dichloromethane at 0 - 30℃; for 1h; Inert atmosphere;
72.7%
(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-[(tert butyldiphenylsilyl)oxy]propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoic acid

(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-[(tert butyldiphenylsilyl)oxy]propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoic acid

dorzolamide
120279-96-1

dorzolamide

(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1-[(1S)-1-({[(2S,4S)-4-(ethylamino)-2-methyl-1,1-dioxo-2H,3H,4H-1λ6-thieno[2,3-b]thiopyran-6-yl]sulfonyl}carbamoyl)ethoxy]-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl (2S)-2-[(tert-butyldiphenylsilyl)oxy]propanoate

(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1-[(1S)-1-({[(2S,4S)-4-(ethylamino)-2-methyl-1,1-dioxo-2H,3H,4H-1λ6-thieno[2,3-b]thiopyran-6-yl]sulfonyl}carbamoyl)ethoxy]-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl (2S)-2-[(tert-butyldiphenylsilyl)oxy]propanoate

Conditions
ConditionsYield
Stage #1: dorzolamide With N-ethyl-N,N-diisopropylamine In dichloromethane at 0℃; for 0.5h; Inert atmosphere;
Stage #2: (2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-[(tert butyldiphenylsilyl)oxy]propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoic acid With dmap; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In dichloromethane at 0 - 30℃; for 1h;
72%
dorzolamide
120279-96-1

dorzolamide

(S)-2-[(1,1-dimethylethyl)diphenylsilyl]oxypropanoic acid
125941-75-5

(S)-2-[(1,1-dimethylethyl)diphenylsilyl]oxypropanoic acid

(2S)-2-[(tert-butyldiphenylsilyl)oxy]-N-{[(2S,4S)-4-(ethylamino)-2-methyl-1,1-dioxo-2H,3H,4H-1λ6-thieno[2,3-b]thiopyran-6-yl]sulfonyl}propanamide

(2S)-2-[(tert-butyldiphenylsilyl)oxy]-N-{[(2S,4S)-4-(ethylamino)-2-methyl-1,1-dioxo-2H,3H,4H-1λ6-thieno[2,3-b]thiopyran-6-yl]sulfonyl}propanamide

Conditions
ConditionsYield
Stage #1: dorzolamide With N-ethyl-N,N-diisopropylamine In dichloromethane at 0℃; for 0.5h; Inert atmosphere;
Stage #2: (S)-2-[(1,1-dimethylethyl)diphenylsilyl]oxypropanoic acid With dmap; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In dichloromethane at 0 - 30℃; for 1h;
68%
(S)-2-(tert-butyldiphenylsilanyloxy)propionic acid (S)-1-((S)-1-carboxyethoxycarbonyl)ethyl ester

(S)-2-(tert-butyldiphenylsilanyloxy)propionic acid (S)-1-((S)-1-carboxyethoxycarbonyl)ethyl ester

dorzolamide
120279-96-1

dorzolamide

(2S)-1-[(1S)-1-({[(2S,4S)-4-(ethylamino)-2-methyl-1,1-dioxo-2H,3H,4H-1λ6-thieno[2,3-b]thiopyran-6-yl]sulfonyl}carbamoyl)ethoxy]-1-oxopropan-2-yl (2S)-2-[(tert-butyldiphenylsilyl)oxy]propanoate

(2S)-1-[(1S)-1-({[(2S,4S)-4-(ethylamino)-2-methyl-1,1-dioxo-2H,3H,4H-1λ6-thieno[2,3-b]thiopyran-6-yl]sulfonyl}carbamoyl)ethoxy]-1-oxopropan-2-yl (2S)-2-[(tert-butyldiphenylsilyl)oxy]propanoate

Conditions
ConditionsYield
Stage #1: dorzolamide With N-ethyl-N,N-diisopropylamine In dichloromethane at 0℃; for 0.5h; Inert atmosphere;
Stage #2: (S)-2-(tert-butyldiphenylsilanyloxy)propionic acid (S)-1-((S)-1-carboxyethoxycarbonyl)ethyl ester With dmap; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In dichloromethane at 0 - 30℃; for 1h;
68%
(S)-2-(tert-butyl-diphenyl-silanyloxy)-propionic acid (S)-1-[(S)-1-((S)-1-carboxy-ethoxycarbonyl)-ethoxycarbonyl]-ethyl ester

(S)-2-(tert-butyl-diphenyl-silanyloxy)-propionic acid (S)-1-[(S)-1-((S)-1-carboxy-ethoxycarbonyl)-ethoxycarbonyl]-ethyl ester

dorzolamide
120279-96-1

dorzolamide

(2S)-1-{[(2S)-1-[(1S)-1-({[(2S,4S)-4-(ethylamino)-2-methyl-1,1-dioxo-2H,3H,4H-1λ6-thieno[2,3-b]thiopyran-6-yl]sulfonyl}carbamoyl)ethoxy]-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl (2S)-2-[(tert-butyldiphenylsilyl)oxy]propanoate

(2S)-1-{[(2S)-1-[(1S)-1-({[(2S,4S)-4-(ethylamino)-2-methyl-1,1-dioxo-2H,3H,4H-1λ6-thieno[2,3-b]thiopyran-6-yl]sulfonyl}carbamoyl)ethoxy]-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl (2S)-2-[(tert-butyldiphenylsilyl)oxy]propanoate

Conditions
ConditionsYield
Stage #1: dorzolamide With N-ethyl-N,N-diisopropylamine In dichloromethane at 0℃; for 0.5h; Inert atmosphere;
Stage #2: (S)-2-(tert-butyl-diphenyl-silanyloxy)-propionic acid (S)-1-[(S)-1-((S)-1-carboxy-ethoxycarbonyl)-ethoxycarbonyl]-ethyl ester With dmap; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In dichloromethane at 0 - 30℃; for 1h;
65%
(S)-2-(tert-butyl-diphenyl-silanyloxy)-propionic acid (S)-1-[(S)-1-((S)-1-carboxy-ethoxycarbonyl)-ethoxycarbonyl]-ethyl ester

(S)-2-(tert-butyl-diphenyl-silanyloxy)-propionic acid (S)-1-[(S)-1-((S)-1-carboxy-ethoxycarbonyl)-ethoxycarbonyl]-ethyl ester

dorzolamide
120279-96-1

dorzolamide

(S)-2-(tert-butyl-diphenyl-silanyloxy)-propionic acid (S)-1-{(S)-1-[(S)-2-((4S,6S)-4-ethylamino-6-methyl-7,7-dioxo-4,5,6,7-tetrahydro-7λ-6-thieno[2,3-b]thiopyran-2-sulfonylamino)-1-methyl-2-oxo-ethoxycarbonyl]ethoxycarbonyl}ethyl ether

(S)-2-(tert-butyl-diphenyl-silanyloxy)-propionic acid (S)-1-{(S)-1-[(S)-2-((4S,6S)-4-ethylamino-6-methyl-7,7-dioxo-4,5,6,7-tetrahydro-7λ-6-thieno[2,3-b]thiopyran-2-sulfonylamino)-1-methyl-2-oxo-ethoxycarbonyl]ethoxycarbonyl}ethyl ether

Conditions
ConditionsYield
With dmap; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In dichloromethane at 0 - 30℃; for 1h;65%
(S)-2-(tert-butyldiphenylsilanyloxy)propionic acid (S)-1-{(S)-1-[(S)-1-((S)-1-carboxyethoxycarbonyl)ethoxycarbonyl]ethoxycarbonyl}ethyl ester

(S)-2-(tert-butyldiphenylsilanyloxy)propionic acid (S)-1-{(S)-1-[(S)-1-((S)-1-carboxyethoxycarbonyl)ethoxycarbonyl]ethoxycarbonyl}ethyl ester

dorzolamide
120279-96-1

dorzolamide

(2S)-1-{[(2S)-1-{[(2S)-1-[(1S)-1-({[(2S,4S)-4-(ethylamino)-2-methyl-1,1-dioxo-2H,3H,4H-1λ6-thieno[2,3-b]thiopyran-6-yl]sulfonyl}carbamoyl)ethoxy]-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl (2S)-2-[(tert-butyldiphenylsilyl)oxy]propanoate

(2S)-1-{[(2S)-1-{[(2S)-1-[(1S)-1-({[(2S,4S)-4-(ethylamino)-2-methyl-1,1-dioxo-2H,3H,4H-1λ6-thieno[2,3-b]thiopyran-6-yl]sulfonyl}carbamoyl)ethoxy]-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl (2S)-2-[(tert-butyldiphenylsilyl)oxy]propanoate

Conditions
ConditionsYield
Stage #1: dorzolamide With N-ethyl-N,N-diisopropylamine In dichloromethane at 0℃; for 0.5h; Inert atmosphere;
Stage #2: (S)-2-(tert-butyldiphenylsilanyloxy)propionic acid (S)-1-{(S)-1-[(S)-1-((S)-1-carboxyethoxycarbonyl)ethoxycarbonyl]ethoxycarbonyl}ethyl ester With dmap; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In dichloromethane at 0 - 30℃; for 1h;
63%
(S)-2-(tert-butyl-diphenyl-silanyloxy)-propionic acid (S)-1-carboxy-ethyl ester

(S)-2-(tert-butyl-diphenyl-silanyloxy)-propionic acid (S)-1-carboxy-ethyl ester

dorzolamide
120279-96-1

dorzolamide

(S)-2-(tert-butyldiphenylsilanyloxy)propionic acid (S)-2-((4S,6S)-4-ethylamino-6-methyl-7,7-dioxo-4,5,6,7-tetrahydro-7λ*6*-thieno[2,3-b]thiopyran-2-sulfonylamino)-1-methyl-2-oxoethyl ester

(S)-2-(tert-butyldiphenylsilanyloxy)propionic acid (S)-2-((4S,6S)-4-ethylamino-6-methyl-7,7-dioxo-4,5,6,7-tetrahydro-7λ*6*-thieno[2,3-b]thiopyran-2-sulfonylamino)-1-methyl-2-oxoethyl ester

Conditions
ConditionsYield
Stage #1: dorzolamide With N-ethyl-N,N-diisopropylamine In dichloromethane at 0℃; for 0.5h; Inert atmosphere;
Stage #2: (S)-2-(tert-butyl-diphenyl-silanyloxy)-propionic acid (S)-1-carboxy-ethyl ester With dmap; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In dichloromethane at 0 - 30℃; for 1h; Inert atmosphere;
60%
dorzolamide
120279-96-1

dorzolamide

Acetoxyacetyl chloride
13831-31-7

Acetoxyacetyl chloride

{[(2S,4S)-6-{[2-(acetyloxy)acetamido]sulfonyl}-2-methyl-1,1-dioxo-2H,3H,4H-1λ6-thieno[2,3-b]thiopyran-4-yl](ethyl)carbamoyl}methyl acetate

{[(2S,4S)-6-{[2-(acetyloxy)acetamido]sulfonyl}-2-methyl-1,1-dioxo-2H,3H,4H-1λ6-thieno[2,3-b]thiopyran-4-yl](ethyl)carbamoyl}methyl acetate

Conditions
ConditionsYield
Stage #1: dorzolamide With N-ethyl-N,N-diisopropylamine In dichloromethane at 0℃; for 0.5h; Inert atmosphere;
Stage #2: Acetoxyacetyl chloride With dmap In dichloromethane at 0 - 30℃; for 1h; Inert atmosphere;
59.6%
carbonochloridic acid, chloromethyl ester
22128-62-7

carbonochloridic acid, chloromethyl ester

dorzolamide
120279-96-1

dorzolamide

chloromethyl ethyl[(4S,6S)-6-methyl-7,7-dioxo-2-sulfamoyl-4,5,6,7-tetrahydro-7λ6-thieno[2,3-b]thiopyran-4-yl]carbamate

chloromethyl ethyl[(4S,6S)-6-methyl-7,7-dioxo-2-sulfamoyl-4,5,6,7-tetrahydro-7λ6-thieno[2,3-b]thiopyran-4-yl]carbamate

Conditions
ConditionsYield
Stage #1: dorzolamide With N-ethyl-N,N-diisopropylamine In dichloromethane at 0℃; for 0.5h; Inert atmosphere;
Stage #2: carbonochloridic acid, chloromethyl ester In dichloromethane at 0 - 30℃; for 1h; Temperature; Inert atmosphere;
57%
Stage #1: dorzolamide With N-ethyl-N,N-diisopropylamine In dichloromethane at 25 - 30℃; for 0.5h;
Stage #2: carbonochloridic acid, chloromethyl ester In dichloromethane at 0 - 5℃; for 1h;
2-(2-{[4-(tert-butoxy)-4-oxobutanoyl]oxy}acetamido)acetic acid

2-(2-{[4-(tert-butoxy)-4-oxobutanoyl]oxy}acetamido)acetic acid

dorzolamide
120279-96-1

dorzolamide

1-tert-butyl 4-{[({[(2S,4S)-4-(ethylamino)-2-methyl-1,1-dioxo-2H,3H,4H-1λ6-thieno[2,3-b]thiopyran-6-yl]sulfonyl}carbamoyl)methyl]carbamoyl}methyl butanedioate

1-tert-butyl 4-{[({[(2S,4S)-4-(ethylamino)-2-methyl-1,1-dioxo-2H,3H,4H-1λ6-thieno[2,3-b]thiopyran-6-yl]sulfonyl}carbamoyl)methyl]carbamoyl}methyl butanedioate

Conditions
ConditionsYield
With dmap; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; N-ethyl-N,N-diisopropylamine In dichloromethane at 0 - 30℃; for 4h; Inert atmosphere;50%
4-{[(acetyloxy)acetyl]oxy}butanoic acid

4-{[(acetyloxy)acetyl]oxy}butanoic acid

dorzolamide
120279-96-1

dorzolamide

3-({[(2S,4S)-4-(ethylamino)-2-methyl-1,1-dioxo-6-sulfamoyl-2H,3H,4H-1λ6-thieno[2,3-b]thiopyran-6-yl]sulfonyl}carbamoyl)propyl 2-(acetyloxy)acetate

3-({[(2S,4S)-4-(ethylamino)-2-methyl-1,1-dioxo-6-sulfamoyl-2H,3H,4H-1λ6-thieno[2,3-b]thiopyran-6-yl]sulfonyl}carbamoyl)propyl 2-(acetyloxy)acetate

Conditions
ConditionsYield
With dmap; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; N-ethyl-N,N-diisopropylamine In dichloromethane at 0 - 30℃; for 1h; Inert atmosphere;48%
[({[(acetyloxy)acetyl]oxy}acetyl)(methyl)amino]acetic acid

[({[(acetyloxy)acetyl]oxy}acetyl)(methyl)amino]acetic acid

dorzolamide
120279-96-1

dorzolamide

{[({[(2S,4S)-4-(ethylamino)-2-methyl-1,1-dioxo-2H,3H,4H-1λ6-thieno[2,3-b]thiopyran-6-yl]sulfonyl}carbamoyl)methyl](methyl)carbamoyl}methyl 2-(acetyloxy)acetate

{[({[(2S,4S)-4-(ethylamino)-2-methyl-1,1-dioxo-2H,3H,4H-1λ6-thieno[2,3-b]thiopyran-6-yl]sulfonyl}carbamoyl)methyl](methyl)carbamoyl}methyl 2-(acetyloxy)acetate

Conditions
ConditionsYield
With dmap; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; N-ethyl-N,N-diisopropylamine In dichloromethane at 0 - 30℃; for 2h; Inert atmosphere;45.1%
(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-(acetyloxy)propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy} propanoic acid

(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-(acetyloxy)propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy} propanoic acid

dorzolamide
120279-96-1

dorzolamide

(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1-[(1S)-1-({[(2S,4S)-4-(ethylamino)-2-methyl-1,1-dioxo-2H,3H,4H-1λ6-thieno[2,3-b]thiopyran-6-yl]sulfonyl}carbamoyl)ethoxy]-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl (2S)-2-(acetyloxy)propanoate

(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1-[(1S)-1-({[(2S,4S)-4-(ethylamino)-2-methyl-1,1-dioxo-2H,3H,4H-1λ6-thieno[2,3-b]thiopyran-6-yl]sulfonyl}carbamoyl)ethoxy]-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl (2S)-2-(acetyloxy)propanoate

Conditions
ConditionsYield
Stage #1: dorzolamide With N-ethyl-N,N-diisopropylamine In dichloromethane at 0℃; for 0.5h; Inert atmosphere;
Stage #2: (2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-(acetyloxy)propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy} propanoic acid With dmap; benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In dichloromethane at 0 - 30℃; for 2h; Inert atmosphere;
42%
octadecanoic acid (S)-1-{(S)-1-[(S)-1-((S)-1-carboxyethoxycarbonyl)ethoxy carbonyl]ethoxycarbonyl}ethyl ester

octadecanoic acid (S)-1-{(S)-1-[(S)-1-((S)-1-carboxyethoxycarbonyl)ethoxy carbonyl]ethoxycarbonyl}ethyl ester

dorzolamide
120279-96-1

dorzolamide

octadecanoic acid (S)-1-((S)-1-{(S)-1-[(S)-2-(4-ethylamino-6-methyl-7,7-dioxo-4,5,6,7-tetrahydro-7λ*6*-thieno[2,3-b]thiopyran-2-sulfonylamino)-1-methyl-2-oxoethoxycarbonyl]ethoxycarbonyl}ethoxycarbonyl)ethyl ester

octadecanoic acid (S)-1-((S)-1-{(S)-1-[(S)-2-(4-ethylamino-6-methyl-7,7-dioxo-4,5,6,7-tetrahydro-7λ*6*-thieno[2,3-b]thiopyran-2-sulfonylamino)-1-methyl-2-oxoethoxycarbonyl]ethoxycarbonyl}ethoxycarbonyl)ethyl ester

Conditions
ConditionsYield
Stage #1: dorzolamide With N-ethyl-N,N-diisopropylamine In dichloromethane at 0℃; for 0.5h; Inert atmosphere;
Stage #2: octadecanoic acid (S)-1-{(S)-1-[(S)-1-((S)-1-carboxyethoxycarbonyl)ethoxy carbonyl]ethoxycarbonyl}ethyl ester With dmap; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In dichloromethane at 0 - 30℃; for 1h; Inert atmosphere;
41%
acetic anhydride
108-24-7

acetic anhydride

dorzolamide
120279-96-1

dorzolamide

N-ethyl-N-[(4S,6S)-6-methyl-7,7-dioxo-2-sulfamoyl-4,5,6,7-tetrahydro-7λ6-thieno[2,3-b]thiopyran-4-yl]acetamide

N-ethyl-N-[(4S,6S)-6-methyl-7,7-dioxo-2-sulfamoyl-4,5,6,7-tetrahydro-7λ6-thieno[2,3-b]thiopyran-4-yl]acetamide

Conditions
ConditionsYield
Stage #1: dorzolamide With triethylamine In dichloromethane at 0℃; for 0.5h; Inert atmosphere;
Stage #2: acetic anhydride In dichloromethane at 0 - 30℃; for 1h; Inert atmosphere;
40%
(S)-2-((S)-2-{(S)-2-[(S)-2-((S)-2-acetoxypropionyloxy)propionyloxy]propionyloxy}propionyloxy)propionic acid

(S)-2-((S)-2-{(S)-2-[(S)-2-((S)-2-acetoxypropionyloxy)propionyloxy]propionyloxy}propionyloxy)propionic acid

dorzolamide
120279-96-1

dorzolamide

(2S)-1-{[(2S)-1-{[(2S)-1-[(1S)-1-({[(2S,4S)-4-(ethylamino)-2-methyl-1,1-dioxo-2H,3H,4H-1λ6-thieno[2,3-b]thiopyran-6-yl]sulfonyl}carbamoyl)ethoxy]-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl (2S)-2-(acetyloxy)propanoate

(2S)-1-{[(2S)-1-{[(2S)-1-[(1S)-1-({[(2S,4S)-4-(ethylamino)-2-methyl-1,1-dioxo-2H,3H,4H-1λ6-thieno[2,3-b]thiopyran-6-yl]sulfonyl}carbamoyl)ethoxy]-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl (2S)-2-(acetyloxy)propanoate

Conditions
ConditionsYield
Stage #1: dorzolamide With N-ethyl-N,N-diisopropylamine In dichloromethane at 0℃; for 0.5h; Inert atmosphere;
Stage #2: (S)-2-((S)-2-{(S)-2-[(S)-2-((S)-2-acetoxypropionyloxy)propionyloxy]propionyloxy}propionyloxy)propionic acid With dmap; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In dichloromethane at 0 - 30℃; for 1h;
38%
(2S)-2-{[(2S)-2-[(4-{[(3Z)-3-[(4-{[2-(diethylamino)ethyl]carbamoyl}-3,5-dimethyl-1H-pyrrol-2-yl)methylidene]-2-oxo-2,3-dihydro-1H-indol-5-yl]oxy}-4-oxobutanoyl)oxy]propanoyl]oxy}propanoic acid

(2S)-2-{[(2S)-2-[(4-{[(3Z)-3-[(4-{[2-(diethylamino)ethyl]carbamoyl}-3,5-dimethyl-1H-pyrrol-2-yl)methylidene]-2-oxo-2,3-dihydro-1H-indol-5-yl]oxy}-4-oxobutanoyl)oxy]propanoyl]oxy}propanoic acid

dorzolamide
120279-96-1

dorzolamide

(3Z)-3-[(4-{[2-(diethylamino)ethyl]carbamoyl}-3,5-dimethyl-1H-pyrrol-2-yl)methylidene]-2-oxo-2,3-dihydro-1H-indol-5-yl (2S)-1-[(1S)-1-({[(2S,4S)-4-(ethylamino)-2-methyl-1,1-dioxo-2H,3H,4H-1λ6-thieno[2,3-b]thiopyran-6-yl]sulfonyl}carbamoyl)ethoxy]-1-oxopropan-2-yl butanedioate

(3Z)-3-[(4-{[2-(diethylamino)ethyl]carbamoyl}-3,5-dimethyl-1H-pyrrol-2-yl)methylidene]-2-oxo-2,3-dihydro-1H-indol-5-yl (2S)-1-[(1S)-1-({[(2S,4S)-4-(ethylamino)-2-methyl-1,1-dioxo-2H,3H,4H-1λ6-thieno[2,3-b]thiopyran-6-yl]sulfonyl}carbamoyl)ethoxy]-1-oxopropan-2-yl butanedioate

Conditions
ConditionsYield
Stage #1: dorzolamide With N-ethyl-N,N-diisopropylamine In dichloromethane at 0℃; for 0.5h; Inert atmosphere;
Stage #2: (2S)-2-{[(2S)-2-[(4-{[(3Z)-3-[(4-{[2-(diethylamino)ethyl]carbamoyl}-3,5-dimethyl-1H-pyrrol-2-yl)methylidene]-2-oxo-2,3-dihydro-1H-indol-5-yl]oxy}-4-oxobutanoyl)oxy]propanoyl]oxy}propanoic acid With dmap; benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In dichloromethane at 0 - 30℃; for 2h;
38%
succinic acid (S)-1-{(S)-1-[(S)-1-((S)-1-carboxyethoxycarbonyl)ethoxycarbonyl]ethoxycarbonyl}ethyl ester 3-[1-[4-(2-diethylaminoethylcarbamoyl)-3,5-dimethyl-1H-pyrrol-2-yl]-meth-(Z)-ylidene]-2-oxo-2,3-dihydro-1H-indol-5-yl ester

succinic acid (S)-1-{(S)-1-[(S)-1-((S)-1-carboxyethoxycarbonyl)ethoxycarbonyl]ethoxycarbonyl}ethyl ester 3-[1-[4-(2-diethylaminoethylcarbamoyl)-3,5-dimethyl-1H-pyrrol-2-yl]-meth-(Z)-ylidene]-2-oxo-2,3-dihydro-1H-indol-5-yl ester

dorzolamide
120279-96-1

dorzolamide

(3Z)-3-[(4-{[2-(diethylamino)ethyl]carbamoyl}-3,5-dimethyl-1H-pyrrol-2-yl)methylidene]-2-oxo-2,3-dihydro-1H-indol-5-yl (2S)-1-{[(2S)-1-{[(2S)-1-[(1S)-1-({[(2S,4S)-4-(ethylamino)-2-methyl-1,1-dioxo-2H,3H,4H-1λ6-thieno[2,3-b]thiopyran-6-yl]sulfonyl}carbamoyl)ethoxy]-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl butanedioate

(3Z)-3-[(4-{[2-(diethylamino)ethyl]carbamoyl}-3,5-dimethyl-1H-pyrrol-2-yl)methylidene]-2-oxo-2,3-dihydro-1H-indol-5-yl (2S)-1-{[(2S)-1-{[(2S)-1-[(1S)-1-({[(2S,4S)-4-(ethylamino)-2-methyl-1,1-dioxo-2H,3H,4H-1λ6-thieno[2,3-b]thiopyran-6-yl]sulfonyl}carbamoyl)ethoxy]-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl butanedioate

Conditions
ConditionsYield
Stage #1: dorzolamide With N-ethyl-N,N-diisopropylamine In dichloromethane at 0℃; for 0.5h; Inert atmosphere;
Stage #2: succinic acid (S)-1-{(S)-1-[(S)-1-((S)-1-carboxyethoxycarbonyl)ethoxycarbonyl]ethoxycarbonyl}ethyl ester 3-[1-[4-(2-diethylaminoethylcarbamoyl)-3,5-dimethyl-1H-pyrrol-2-yl]-meth-(Z)-ylidene]-2-oxo-2,3-dihydro-1H-indol-5-yl ester With dmap; benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In dichloromethane at 0 - 30℃; for 2h;
38%
2-{2-[3-(butylamino)-4-phenoxy-5-sulfamoylbenzoyloxy]-N-methylacetamido}acetic acid

2-{2-[3-(butylamino)-4-phenoxy-5-sulfamoylbenzoyloxy]-N-methylacetamido}acetic acid

dorzolamide
120279-96-1

dorzolamide

C32H41N5O11S4

C32H41N5O11S4

Conditions
ConditionsYield
With dmap; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; N-ethyl-N,N-diisopropylamine In dichloromethane at 0 - 30℃; for 16h;38%

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