Direct and Regioselective C-H Alkenylation of Tetrahydropyrido[1,2-a]pyrimidines

被引:69
作者
Cheng, Dachen [1 ]
Gallagher, Timothy [1 ]
机构
[1] Univ Bristol, Sch Chem, Bristol BS8 1TS, Avon, England
关键词
PALLADIUM(II) ACETATE; DIRECT ARYLATION; 2(1H)-PYRIDONE DERIVATIVES; BOND FUNCTIONALIZATION; AROMATIC SUBSTITUTION; HECK REACTION; OLEFINS; ACTIVATION; ARENES; INDOLES;
D O I
10.1021/ol900627q
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
The electrophilic C-H palladation and Heck-type alkenylation of the tetrahydro[1,2-a]pyrimidine scaffold leads to exclusive formation of the C(7) adducts, and this palladium-catalyzed process is applicable to a broad range of alkenyl components. Mechanistic studies suggest that palladation is selective for C(7), and there was no evidence for C(9) metalation; the latter corresponds to the pathway observed previously with N-methylpyridone.
引用
收藏
页码:2639 / 2641
页数:3
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