SYNTHESIS METHOD FOR CANDESARTAN CILEXETIL INTERMEDIATE

Title:

SYNTHESIS METHOD FOR CANDESARTAN CILEXETIL INTERMEDIATE

Document Type and Number:

WIPO Patent Application WO/2020/140193

Kind Code:

A1

Abstract:

A synthesis method for a candesartan cilexetil intermediate represented by formula (II). The method comprises: (1) dissolving a compound represented by formula (IV) to an aprotic solvent to obtain a first mixed solution, and dissolving a phase transfer catalyst and an azidation reagent to water to obtain a second mixed solution; (2) dropping the first mixed solution to the second mixed solution for azidation reaction, and after the reaction is ended, standing and layering same to obtain an organic phase containing a compound represented by formula (V); (3) dropping the obtained organic phase containing the compound represented by formula (V) to tertiary butyl alcohol for rearrangement reaction, and after the reaction is ended, concentrating same to obtain a solid or oily material, then adding a crystallizing solvent to the obtained solid or oily material for recrystallization, and separating same to obtain a crystal, i.e., the candesartan cilexetil intermediate represented by formula (II). The synthesis method of the present application does not require the use of a DMF solvent, is safe and environmentally friendly, and reduces generation of ammonia nitrogen wastewater.

Inventors:

TU GUOLIANG (CN)
HUANG JIANSHENG (CN)
ZHANG LU (CN)
YANG TAO (CN)
LIANG ZUNJUN (CN)

Application Number:

PCT/CN2019/070055

Publication Date:

July 09, 2020

Filing Date:

January 02, 2019

Export Citation:

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Assignee:

LINHAI HUANAN CHEMICAL CO LTD (CN)
ZHEJIANG HUAHAI PHARM CO LTD (CN)

International Classes:

C07C67/30; C07C69/76

Domestic Patent References:

WO2011145100A1	2011-11-24
WO2013186792A2	2013-12-19

Foreign References:

CN101880241A	2010-11-10
CN104876877A	2015-09-02
CN1425654A	2003-06-25
CN102408353A	2012-04-11
US5196444A	1993-03-23

Other References: