93479-97-1 (格列美脲,Glimepiride)

_97%

反应条件：

1.1 Reagents: Triethylamine Solvents: Dichloromethane ; 7 h, rt

参考文献：

Preparation method of glimepiride for anti-diabetes drug

, China, , ,

合成路线：1 步

_95%

反应条件：

1.1 Solvents: tert-Butyl methyl ether
1.2 Solvents: Toluene , Cyclohexanone , tert-Butyl methyl ether ; 10 h, 30 °C

参考文献：

Method for preparing hypoglycemic drug glimepiride

, China, , ,

合成路线：1 步

318515-70-7

2523-55-9

_95%

反应条件：

1.1 Reagents: 4-(Dimethylamino)pyridine Solvents: Toluene ; rt → reflux

参考文献：

Method for the manufacture of compounds related to the class of substituted sulfonyl urea antidiabetics

, European Patent Organization, , ,

合成路线：1 步

_90%

反应条件：

1.1 Reagents: Potassium carbonate Solvents: Tetrahydrofuran ; 1 - 2 h, rt → 65 °C
1.2 Solvents: Toluene ; 10 - 12 h, 60 - 65 °C; cooled
1.3 Reagents: Ammonia Solvents: Methanol ; pH 10 - 12
1.4 Reagents: Acetic acid ; pH 5.5 - 6.0, 25 - 30 °C

参考文献：

A process for purification of glimepiride

, India, , ,

合成路线：1 步

_90%

反应条件：

1.1 Reagents: Potassium carbonate Solvents: Acetone , Methyl ethyl ketone ; 30 min, rt → reflux
1.2 5 - 6 h, reflux
1.3 Reagents: Hydrochloric acid Solvents: Water ; pH 6

参考文献：

Preparation of glimepiride

, China, , ,

合成路线：1 步

321655-42-9

_89%

反应条件：

1.1 Reagents: Sodium methoxide Solvents: Dimethyl sulfoxide
1.2 Reagents: Water

参考文献：

Improved process for the preparation of benzenesulfonylureas used as second-generation oral hypoglycemic agents

, World Intellectual Property Organization, , ,

合成路线：1 步

_86%

反应条件：

1.1 Reagents: Potassium carbonate Solvents: Acetone ; 1 h, 55 - 60 °C
1.2 Solvents: Toluene ; 12 h, reflux
1.3 Reagents: Acetic acid Solvents: Water ; pH 5.5 - 6, 20 - 25 °C

参考文献：

A novel process for preparation of substantially pure glimepiride

, World Intellectual Property Organization, , ,

合成路线：1 步

1988102-95-9

_85%

反应条件：

1.1 Reagents: 1,8-Diazabicyclo[5.4.0]undec-7-ene Solvents: Acetonitrile ; 5 h, reflux

参考文献：

An Efficient and Practical Process for the Synthesis of Glimepiride

Tanwar, Dinesh Kumar; Surendrabhai, Vaghela Ravikumar; Gill, Manjinder Singh, Synlett, 2017, 28(18), 2495-2498

合成路线：1 步

318515-70-7

2523-55-9

_85%

反应条件：

1.1 Solvents: Toluene

参考文献：

Studies on synthetic process of glimepiride, new hypoglycemic agent

Deng, Yong; Zhong, Yuguo; Tang, Weigao; Zhong, Zhicheng, Zhongguo Yaowu Huaxue Zazhi, 2000, 10(2), 134-137

合成路线：1 步

_84%

反应条件：

1.1 Solvents: Toluene ; rt
1.2 rt → reflux; 4 h, reflux; reflux → 15 °C

参考文献：

Process for preparing glimepiride and corresponding intermediate

, Czech Republic, , ,

合成路线：1 步

_83%

反应条件：

1.1 Reagents: Potassium carbonate Solvents: Acetone ; 6 h, reflux
1.2 6 h, reflux; reflux → rt
1.3 Reagents: Hydrochloric acid Solvents: Water ; pH 2

参考文献：

studies on the preparation of glimepiride

Liu, Sheng-gao, Shandong Huagong, 2009, 38(6), 14-15

合成路线：1 步

_83%

反应条件：

1.1 Reagents: Triethylamine , Ethyl chloroformate Solvents: Dichloromethane ; 2 h, 20 - 25 °C
1.2 Reagents: Acetic acid Solvents: Water ; pH 4 - 4.2; 30 min
1.3 Reagents: 4-(Dimethylamino)pyridine Solvents: Toluene ; rt → reflux; 3 h, reflux; reflux → 30 °C; 3 h, 25 - 30 °C

参考文献：

An improved process for the preparation of N-{2-[4-(aminosulfonyl)phenyl]ethyl}-3-ethyl-4-methyl-2-oxo-2,5-dihydro-1H-pyrrole-1-carboxamide, a key intermediate in the synthesis of glimepiride

, India, , ,

合成路线：1 步

_82%

反应条件：

1.1 Reagents: Diisopropylethylamine Solvents: Dimethylformamide ; 3 h, rt → 25 °C
1.2 Solvents: Dimethylformamide ; overnight, heated

参考文献：

Preparation method of glimepiride

, China, , ,

合成路线：1 步

_80%

反应条件：

1.1 Reagents: Potassium carbonate Solvents: Acetonitrile ; rt → 60 °C
1.2 6 h, 50 - 60 °C
1.3 Reagents: Hydrochloric acid Solvents: Water ; pH 1 - 2, 20 - 25 °C

参考文献：

Synthetic preparation of glimepiride bulk drug

, China, , ,

合成路线：1 步

_75%

反应条件：

1.1 Reagents: Potassium carbonate Solvents: Acetone ; 6 h, reflux
1.2 8 h, reflux; reflux → rt
1.3 Reagents: Hydrochloric acid Solvents: Water ; pH 1 - 2

参考文献：

Synthesis of 3-ethyl-2,5-dihydro-4-methyl-N-[2-[4-[[[[(trans-4-methylcyclohexyl)amino]carbonyl]amino]sulfonyl]phenyl]ethyl]-2-oxo-1H-pyrrole-1-carboxamide (glimepiride)

Liu, Zhanke; Yang, Xinwu; Lu, Qihui; Wang, Xiaoguang; Liu, Zhiling, Jingxi Huagong Zhongjianti, 2006, 36(3), 16-18

合成路线：1 步

_52%