Direct, Regioselective N-Alkylation of 1,3-Azoles

被引：37

作者：

Chen, Shuai ^{[1
]}

Graceffa, Russell F. ^{[1
]}

Boezio, Alessandro A. ^{[1
]}

机构：

[1] Amgen Inc, Med Chemsitry Dept, Cambridge, MA 02142 USA

来源：

ORGANIC LETTERS | 2016年 / 18卷 / 01期

关键词：

9-SUBSTITUTED TETRAHYDRODIAZEPINOPURINES; BIOLOGICAL EVALUATION; METHYLATION; INHIBITORS; PURINES; ANALOGS; DERIVATIVES; IMIDAZOLES; NUCLEOSIDE;

D O I：

10.1021/acs.orglett.5b02994

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Regioselective N-alkylation of 1,3-azoles is a valuable transformation. Organomagnesium reagents were discovered to be competent bases to affect regioselective alkylation of various 1,3-azoles. Counterintuitively, substitution selectively occurred at the more sterically hindered nitrogen atom. Numerous examples are provided, on varying 1,3-azole scaffolds, with yields ranging from 25 to 95%.

引用

页码：16 / 19

页数：4

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