发明名称 |
Improved method of making nevirapine. |
摘要 |
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. |
申请公布号 |
ZA200407107(B) |
申请公布日期 |
2005.05.24 |
申请号 |
ZA20040007107 |
申请日期 |
2004.09.06 |
申请人 |
BOEHRINGER INGELHEIM CHEMICALS, INC. |
发明人 |
BOSWELL, ROBERT, F., JR;GUPTON, BERNARD, FRANKLIN;LO, YOUNG, S. |
分类号 |
C07D213/78;C07D213/80;C07D213/803;C07D213/82;C07D213/85;C07D471/10;C07D471/14 |
主分类号 |
C07D213/78 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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