Patent · US Expired

Method for synthesizing leflunomide

US6723855B2 · kind B2 · utility

1Cited by
6References
26Claims
0Family size

Assignee

Inventors

Key dates

Filing dateFeb 8, 2001
Grant dateApr 20, 2004
Priority date
Expiry dateMar 20, 2021

Classification

  • Technology area (CPC A)Human Necessities
  • CPC primaryA61P37/06
  • WIPO fieldPharmaceuticals
  • WIPO sectorChemistry

Abstract

A process for synthesizing leflunomide from 5-methylisoxazole-4-carboxylic acid and 4-trifluoromethylaniline is provided in which the carboxylic acid group of 5-methylisoxazole-4-carboxylic acid is chlorinated, forming 5-methylisoxazole-4-carboxylic acid chloride. The acid chloride is then reacted without intermediate distillation with 4-trifluoromethylaniline in the presence of an alkali metal or alkaline-earth metal bicarbonate acid scavenger.

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