SYNTHESIS OF NEVIRAPINE AND ITS MAJOR METABOLITE

被引:19
作者
GROZINGER, KG
FUCHS, V
HARGRAVE, KD
MAULDIN, S
VITOUS, J
CAMPBELL, S
ADAMS, J
机构
[1] Boehringer Ingelheim Pharmaceuticals, Inc, Process Chemistry Research, Ridgebury, Connecticut, 06877-0368
[2] Eli Lilly, Indianapolis, Indiana
[3] MyoGenics Inc, Cambridge, Massachusetts, 02139
关键词
D O I
10.1002/jhet.5570320144
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Several synthetic methods were developed during the process optimization for the large scale synthesis of nevirapine (1), a non-nucleoside inhibitor of HIV-1 Reverse Transcriptase. The synthesis of its putative major metabolite 11-cyclopropyl-5,11-dihydro-4-hydroxymethyl-6H-[3,2-b:2',3'-e][1,4]diazepin-6-one (2) and the oxidation of 2 to the corresponding aldehyde 3, are described.
引用
收藏
页码:259 / 263
页数:5
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