Method for preparing a sitagliptin intermediate

Number of patents in Portfolio can not be more than 2000

United States of America Patent

PATENT NO 9745309
APP PUB NO 20160229859A1
SERIAL NO

15021066

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Abstract

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The present invention provides a method for preparing an intermediate compound of sitagliptin represented by formula I. The preparation method comprises: dissolving a compound represented by formula II into an organic solvent; and under the catalysis of fatty acid and effect of chlorosilane, performing a reduction reaction of carbon-carbon double bonds, so as to obtain the intermediate compound of sitagliptin represented by formula I, R being methyl or formoxyl. The preparation method of the present invention avoids precious metal as a catalyst, and accordingly, the cost is low, the post-treatment is simple, the product has a high yield, chemical purity and optical purity, and de % is greater than 99.6%, and the preparation method can be used in synthesis of sitagliptin and is suitable for industrial production.

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Patent Owner(s)

Patent OwnerAddress
SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRY200040 NO 1320 WEST BEIJING ROAD SHANGHAI SHANGHAI CITY SHANGHAI CITY 200040

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Cai, Zhengyan Xinchang County, CN 3 0
Lin, Kuaile Xinchang County, CN 1 0
Pan, Jing Xinchang County, CN 99 861
Shen, Dadong Xinchang County, CN 6 0
Wu, Guofeng Xinchang County, CN 14 3
Yue, Lirong Xinchang County, CN 1 0
Zhou, Weicheng Xinchang County, CN 10 4

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