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

来源：

TETRAHEDRON LETTERS | 1996年 / 37卷 / 25期

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.

引用

页码：4289 / 4292

页数：4

共 4 条

[1] PALLADIUM-CATALYZED REACTIONS IN THE SYNTHESIS OF 3-SUBSTITUTED AND 4-SUBSTITUTED INDOLES .2. TOTAL SYNTHESIS OF THE N-ACETYL METHYL-ESTER OF (+/-)-CLAVICIPITIC ACIDS
HARRINGTON, PJ
HEGEDUS, LS
MCDANIEL, KF
[J]. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1987, 109 (14) : 4335 - 4338
[2] HOPKINS S J, 1992, Drugs of Today, V28, P155
[3] LEE WS, 1993, BRAIN RES, V626, P303
[4] THE SYNTHESIS OF A CONFORMATIONALLY RESTRICTED ANALOG OF THE ANTIMIGRAINE DRUG SUMATRIPTAN
MACOR, JE
BLANK, DH
POST, RJ
RYAN, K
[J]. TETRAHEDRON LETTERS, 1992, 33 (52) : 8011 - 8014

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