Preparation method of trandolapril midbody (2S, 3aR, 7aS)-octahydro-1H-indole-2-carboxylic acid

A technology for trandolapril and intermediates, which is applied in the field of intermediates for the preparation of drugs, can solve problems such as difficult separation and purification processes, and achieve the effects of low cost, easy control, and simple process

Inactive Publication Date: 2013-09-11
大连鼎燕医药化工有限公司 +1
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  • Preparation method of trandolapril midbody (2S, 3aR, 7aS)-octahydro-1H-indole-2-carboxylic acid

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Abstract

The invention discloses a preparation method of trandolapril midbody (2S, 3aR, 7aS)-octahydro-1H-indole-2-carboxylic acid, and the preparation method comprises the following steps of: preparing 3-chlorine-2-amino-propionic acid methyl ester hydrochloride by using phosphorous pentachloride and dichloromethane; preparing 3-chlorine-2-acetyl amino-propionic acid methyl ester hydrochloride by using the 3-chlorine-2-amino-propionic acid methyl ester hydrochloride, methylbenzene and acetyl chloride; preparing 2,3,4,5,6,7-hexahydro-1H-indole-2-carboxylic acid by using the 3-chlorine-2-acetyl amino-propionic acid methyl ester hydrochloride, DMF (Dimethyl Formamide) and 1-pyrrole cyclohexene; preparing (2S)-octahydro-1H-indole-2-methyl carboxylat by using the 2,3,4,5,6,7-hexahydro-1H-indole-2-carboxylic acid, methanol and palladium on carbon; preparing the (2S, 3aR, 7aS)-octahydro-1H-indole-2-carboxylic acid by using the (2S)-octahydro-1H-indole-2-methyl carboxylat and the methanol. Compared with the prior art, the preparation method of the trandolapril midbody (2S, 3aR, 7aS)-octahydro-1H-indole-2-carboxylic acid, which is disclosed by the invention, has the advantages of easiness and convenience for process, easiness for control, safety, reliability and low cost.

Description

technical field The invention relates to an intermediate for the preparation of medicines, in particular to a method for preparing a trandolapril intermediate (2S, 3aR, 7aS)-octahydro-1H-indole-2-carboxylic acid. Background technique The chemical name of trandolapril is (2S, 3aR, 7aS)-1-[(2S)-2-[(1S)-1-(ethoxycarbonyl)-3-phenylpropyl]amino]-1-oxo Propyl]octahydro-1H-indole-2-carboxylic acid is a long-acting angiotensin-converting enzyme inhibitor (ACEI) developed by Roussel Uclaf Company in Germany. Clinical indications for hypertension, congestive heart failure and myocardial infarction. (2S, 3aR, 7aS)-octahydro-1H-indole-2-carboxylic acid is the most important intermediate for the preparation of trandolapril. Many multinational companies in the world have conducted in-depth research on its synthesis process. So far, it has There are 5 main process routes with their respective pros and cons as follows: Route 1: In U.S. Patent No. 6,599,318, 1,1,3,3,-tetramethoxypropa...

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IPC IPC(8): C07D209/42
Inventor 张勇鹿军汪洋范莉莉吴冬辉李艳凤孙立芹薛丽红李德龙
Owner 大连鼎燕医药化工有限公司
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