Patent · US Active

Method for preparing a sitagliptin intermediate

US9745309B2 · kind B2 · utility

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12Claims
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Key dates

Filing dateSep 9, 2014
Grant dateAug 29, 2017
Priority date
Expiry dateSep 9, 2034

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07B2200/13
  • WIPO fieldOrganic fine chemistry
  • WIPO sectorChemistry

Abstract

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.

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.