Title:
ネビラピンの改良された製造方法
Document Type and Number:
Japanese Patent JP2005533083
Kind Code:
A
Abstract:
A process for making nevirapine, comprising the following steps:(a) reacting a 2-halo-3-pyridinecarbonitrile of the formulawherein 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 formulawherein 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.
Inventors:
Bothwell Robert F Junior
Gapton Bernard Franklin
Low Yang S
Gapton Bernard Franklin
Low Yang S
Application Number:
JP2004517609A
Publication Date:
November 04, 2005
Filing Date:
June 02, 2003
Export Citation:
Assignee:
Boehringer Ingelheim Chemicals, Inc.
International Classes:
C07D213/78; C07D213/80; C07D213/803; C07D213/82; C07D213/85; C07D471/10; C07D471/14; (IPC1-7): C07D471/10; C07D213/80; C07D213/803; C07D213/82
Attorney, Agent or Firm:
Sadao Kumakura
Nobuo Ogawa
Atsushi Hakoda
Kenji Asai
Koji Hirayama
Nobuo Ogawa
Atsushi Hakoda
Kenji Asai
Koji Hirayama