Combinatorial synthesis of libraries of indole derivatives

被引：11

作者：

Nettekoven, M ^{[1
]}

机构：

[1] F Hoffmann La Roche & Co Ltd, Pharmaceut Res, Discovery Chem Lead Generat, CH-4070 Basel, Switzerland

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 16期

关键词：

D O I：

10.1016/S0960-894X(01)00393-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis of two indole derivative libraries is described. 2-Acyl-3-amino-indoles 4 can easily be accessed by treatment of the intermediates 3 with bases in a one-pot reaction sequence whereas the reaction of the isolated intermediates 5 (R-3 =aromatic-, heteroaromatic, or cycloalkyl) with acid chlorides yielded the novel indole derivatives 6. The products were purified by reversed phase column chromatography and obtained in multi-milligram quantities in acceptable yields. (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：2169 / 2171

页数：3

共 11 条

[1]

[Anonymous], INDOLES BEST SYNTHET

[2]

ANTONENKO VV, 1999, COMB CHEM TECHNOL, V204, P4

[3]

Balkenhohl F, 1996, ANGEW CHEM INT EDIT, V35, P2289

[4] Application of combinatorial technologies for catalyst design and development [J].