N-amination of pyrrole and indole heterocycles with monochloramine (NH2Cl)

被引：62

作者：

Hynes, J ^{[1
]}

Doubleday, WW

Dyckman, AJ

Godfrey, JD

Grosso, JA

Kiau, S

Leftheris, K

机构：

[1] Bristol Myers Squibb Co, Pharmaceut Res Inst, Dept Discovery Cheem, Princeton, NJ 08543 USA

[2] Bristol Myers Squibb Co, Pharmaceut Res Inst, Dept Proc Res & Dev, Princeton, NJ 08543 USA

[3] Bristol Myers Squibb Co, Pharmaceut Res Inst, Dept Proc Res & Dev, New Brunswick, NJ 08903 USA

来源：

JOURNAL OF ORGANIC CHEMISTRY | 2004年 / 69卷 / 04期

关键词：

D O I：

10.1021/jo035587p

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A survey of several electrophilic ammonia reagents for the N-amination of indole- and pyrrole-containing heterocycles revealed that monochloramine (NH2Cl) is an excellent reagent for this transformation. Pyrroles and indoles containing a variety of substitution were aminated on nitrogen with isolated yields ranging from 45% to 97%.

引用

页码：1368 / 1371

页数：4

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