Patent · US Expired

Method for making nevirapine

US6680383B1 · kind B1 · utility

0Cited by
2References
6Claims
0Family size

Assignee

Inventors

Key dates

Filing dateJun 5, 2003
Grant dateJan 20, 2004
Priority date
Expiry dateJun 5, 2023

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07D471/14
  • WIPO fieldOrganic fine chemistry
  • WIPO sectorChemistry

Abstract

A process for making nevirapine, comprising the following steps:(a) reacting a 2-halo-3-pyridinecarbonitrile of the formula wherein X is a fluorine, chlorine, bromine or iodine atom, preferably chlorine or bromine, with cyclopropylamine, to yield 2-(cyclopropylamino)-3-pyridinecarbonitrile;(b) hydrolyzing the 2-(cyclopropylamino)-3-pyridinecarbonitrile to yield 2-(cyclopropylamino)-3-pyridine carboxylic acid;(c) isolating the 2-(cyclopropylamino)-3-pyridine carboxylic acid from the reaction medium;(e) treating the 2-(cyclopropylamino)-3-pyridine carboxylic acid with a chlorinating agent, to yield 2-(cyclopropylamino)-3-pyridinecarbonyl chloride;(f) reacting the 2-(cyclopropylamino)-3-pyridine carbonyl chloride with a 2-halo-4-methyl-3-pyridinamine of the formula wherein X is a fluorine, chlorine, bromine or iodine atom, preferably chlorine or bromine, to produce an N-(2-halo-4-methyl-3-pyridinyl)-2-(cyclopropylamino)-3-pyridinecarboxamide; and (g) cyclizing the N-(2-halo-4-methyl-3-pyridinyl)-2-(cyclopropylamino)-3-pyridinecarboxamide by treatment with a strong base, to yield nevirapine.

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