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Preparation method for fosinopril and its salt

A sodium salt, controlled technology, applied in the field of preparation of fosinopril and its salt, can solve the problem of low yield

Active Publication Date: 2012-09-05
常州华生制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Generally, the yield of this synthetic method of fosinopril is not high, and there is a need for improvement

Method used

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  • Preparation method for fosinopril and its salt
  • Preparation method for fosinopril and its salt
  • Preparation method for fosinopril and its salt

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-3

[0115] Repeat the steps of Comparative Example 1, wherein the drying method of the present invention is used to dry R-6 so that it has a lower water content.

[0116] The results of Comparative Examples 1-5 and Examples 1-3 are listed in Table 2 below.

[0117] The influence of table 2 different R-6 water content on fosinopril sodium yield

[0118] Example

[0119] Example 1

[0120] It can be seen that, by effectively controlling the water content of (2S, 4S)-4-cyclohexylpyrrolidine-2-carboxylic acid [R-6], the present invention greatly increases the yield of fosinopril.

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Abstract

The present invention discloses a method for preparing fosinopril and salt thereof. By controlling the water content of the prepared intermediate, (2S, 4S)-4-cyclohexylpyrrolidine-2-carboxylate, or using the intermediate with low water content, (2S, 4S)-4-cyclohexylpyrrolidine-2-carboxylate, the yield of the fosinopril or the salt thereof can be increased from approximate 50 percent to more than 70 percent. The control of water content adopts a combined method of vacuum drying and desiccant. The present invention also provides intermediate (2S, 4S)-4-cyclohexylpyrrolidine-2-carboxylate with low water content.

Description

technical field [0001] The present invention relates to the preparation method of fosinopril and its salt, in particular, relates to a preparation method of controlling the water content of its preparation intermediate. Background technique [0002] Angiotensin-converting enzyme converts angiotensin I to angiotensin II, which causes high blood pressure. Fosinopril (for example, trans-4-cyclohexyl-1-[[[2-methyl-1-(1-oxopropoxy)propoxy](4-phenylbutyl)phosphine oxide Base] Acetyl-L-proline sodium salt) is a drug known as an angiotensin-converting enzyme inhibitor (ACE), mainly used in the treatment of hypertension. [0003] The chemical structural formulas of fosinopril and its salts such as sodium salt are as follows. [0004] [0005] Fosinopril Fosinopril Sodium [0006] There are many ways to synthesize fosinopril and its salts, some of which are described in US patents US 4,337,201 and US 4,873,356, US patent application US 2006 / 0160772 A1 and international applicati...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07F9/572C07D207/16
Inventor 钟海涛
Owner 常州华生制药有限公司
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