ImProved synthesis of aIogIiPtin benzoate
sHI Bingyue
GUO Xinliang
WANG Fang
Abstract：Pbjective To improve synthetic process of alogliptin benzoate. Methods Alogliptin benzoate was synthe-sized from 6—chlorine uracil and iodomethane to give 3 —methyl—6 —chlorine uracil,then in the presence of inorganic base with 2—bromine methyl benzonitrile reaction to 2—(6—methyl chloride—3—2,4—dichloro generation—3,4—di-hydro—2 h—pyrimidine—1—methyl)—benzonitrile,which was subjected to displacement with( R)—3—aminopiperidine in the presence of inorganic base. And then salified with benzoic acid to obtain alogliptin benzoate. ResuIts Alogliptin ben-zoate was synthesized. The overall yield was 57. 09%,and its purity was 99. 6%. ConcIusion The improvement reduced toxic,and was economic and environmental. It was suitable for industrial production.
Keywords：Alogliptin benzoateSynthesisImprovement
Publication Date：2015-01-01
Online Publishing Date：2025-08-15(First online date of this platform, not the publication date of the document)
Pages：2( 55-56 )