An improved synthesis of the unique anti-migraine agent CP-122,288: A bromine atom passenger in an intramolecular Heck reaction

被引:26
作者
Macor, JE
Ogilvie, RJ
Wythes, MJ
机构
[1] PFIZER INC,DIV CENT RES,GROTON,CT 06340
[2] PFIZER INC,DIV CENT RES,SANDWICH,KENT,ENGLAND
关键词
D O I
10.1016/0040-4039(96)00322-X
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Utilizing a 2,6-dihromoaniline (6b) in place of the original monobromo aniline in the indole-forming intramolecular Heck reaction allows for a greater than two-fold improvement in the overall yield of CP-122,288. The second bromine is carried through unmolested, forming a 7-bromoindole analog of CP-122,288 (1b). This result might represent a novel approach to 7-substituted indole derivatives. Copyright (C) 1996 Elsevier Science Ltd.
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页码:4289 / 4292
页数:4
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