Synthesis of 4-trifluoromethylpyrido[1,2-a]pyrimidin-2-ones utilizing activated alkynoates

被引:32
|
作者
Harriman, GCB [1 ]
Chi, S [1 ]
Zhang, M [1 ]
Crowe, A [1 ]
Bennett, RA [1 ]
Parsons, I [1 ]
机构
[1] Millennium Pharmaceut Inc, Cambridge, MA 02139 USA
关键词
D O I
10.1016/S0040-4039(03)00700-7
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
The synthesis of the biologically relevant, 4-trifluoromethylpyrido[1,2-a]pyrimidin-2-one 7, is reported. Addition of substituted 2-aminopyridines 5 to activated alkynoates leads to the facile formation of a series of metabolically stable trifluoromethyl substituted pyrido[1,2-a]pyrimidines under mild conditions. (C) 2003 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:3659 / 3662
页数:4
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