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Method for preparing key intermediate of medication for anti AIDS

An anti-AIDS and intermediate technology, applied in the preparation of carboxylate/lactone, organic chemistry, etc., can solve the problems of large amount of three wastes, low total yield, etc. The effect of high purity

Inactive Publication Date: 2009-01-07
ZHEJIANG JIUZHOU PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This method is feasible, but the amount of three wastes to be treated is relatively large, and the total yield is as low as about 35%.

Method used

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  • Method for preparing key intermediate of medication for anti AIDS
  • Method for preparing key intermediate of medication for anti AIDS
  • Method for preparing key intermediate of medication for anti AIDS

Examples

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Embodiment Construction

[0030] The following examples are used to further illustrate the present invention, but not to limit the scope of the present invention.

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Abstract

This invention discloses a method for manufacturing the intermediate of an anti-AIDS drug. The method uses phenyl aldehyde as the raw material, and subjects it to condensation, reduction, Grignard reaction and hydrolysis to obtain (R)-3-hydroxyl-3-(20phenylethyl)-hexanoic acid. The yield is 50-60%.

Description

technical field [0001] The invention belongs to the technical field of chemical industry and pharmacy, and relates to a preparation method of a key intermediate (R)-3-hydroxyl-3-(2-phenylethyl)-hexanoic acid formula (2) compound of anti-HIV drug TIPRANAVIR. Background technique [0002] TIPRANAVIR, a compound of formula (1), is an HIV-1 protease inhibitor. [0003] [0004] (R)-3-Hydroxy-3-(2-phenylethyl)-hexanoic acid, the compound of formula (2), is the key intermediate of TIPRANAVIR. [0005] [0006] The synthetic method of (R)-3-hydroxyl-3-(2-phenylethyl)-hexanoic acid disclosed in the prior art mainly contains the following types: [0007] Described in J.Org.Chem.1998 63,7348-7356 is a starting material with 3-phenylhexanone, then reacts with the lithium salt of ethyl acetate to prepare the 3-hydroxyl-3-( 2-Phenylethyl)-hexanoic acid. (R)-3-Hydroxy-3-(2-phenylethyl)-hexanoic acid was obtained by resolution with (-)norephedrine. According to this method, lithi...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C59/50C07C51/09
Inventor 李文泽张达徐明东梅义将
Owner ZHEJIANG JIUZHOU PHARM CO LTD
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