Synthesis method of candesartan cilexetil

The invention discloses a synthesis method of candesartan cilexetil. The candesartan cilexetil is synthesized by esterification reaction, reduction reaction, carbalkoxylation reaction, nitration reaction, N-alkylation reaction, catalytic hydrogenation reaction, cyclization reaction, hydrolysis react...

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Main Authors QIAO ZAIYIN, CHEN LIYANG, HUANG JIANJUN, YU ZEMIN, HE HAIBING, TU LIANG, JI JIAN, GAO BIN, GE SHAOYONG
Format Patent
LanguageChinese
English
Published 23.01.2013
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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Summary:The invention discloses a synthesis method of candesartan cilexetil. The candesartan cilexetil is synthesized by esterification reaction, reduction reaction, carbalkoxylation reaction, nitration reaction, N-alkylation reaction, catalytic hydrogenation reaction, cyclization reaction, hydrolysis reaction, condensation reaction and de-protection reaction. According to the invention, the start raw material is 2-nitro-benzoic acid, and the synthesis using sodium azide and tetrazole rings is avoided; an activator tetrabutylammonium bromide is used in the condensation reaction, and palladium on carbon is used in the catalytic hydrogenation reaction; the conditions of the whole reaction system are mild, and a proper crystallization solvent is selected; and thus, the production of impurities is reduced, the cost is lowered, the environmental pollution is reduced, the yield and product quality are improved, and the method is suitable for large-scale production.
Bibliography:Application Number: CN20121436639