Patent · US Active

Method for preparing rivaroxaban intermediate

US9079892B2 · kind B2 · utility

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11Claims
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Key dates

Filing dateFeb 22, 2013
Grant dateJul 14, 2015
Priority date
Expiry dateFeb 22, 2033

Classification

  • Technology area (CPC Y)Emerging Cross-Sectional Technologies
  • CPC primaryY02P20/55
  • WIPO fieldOrganic fine chemistry
  • WIPO sectorChemistry

Abstract

A method for preparing a Rivaroxaban intermediate I is presented, including the following step: in a non-protonic solvent, under the effect of lewis acid, performing cyclization reaction on 4-(4-phenyl isocyanate)morpholine-3-ketone (II) and (S)-epoxy compound (III), the reaction temperature ranging from 20° C. to 60° C., where R is amino replaced by amino protecting group. The preparation method of the present invention has a mild condition, a simple process, a low cost, and high efficiency; the product is easy to purify and the method is applicable to industrial production.

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