通过钯催化的C-H活化实现4H-吡啶并[1,2-a]嘧啶-4-酮的区域选择性C3烯基化反应。
Regioselective C3 alkenylation of 4 H-pyrido[1,2-a]pyrimidin-4-ones via palladium-catalyzed C-H activation.
作者信息
Liu Wenjie, Wang Shaohua, Zhang Qi, Yu Jingwen, Li Jiahe, Xie Zhiwei, Cao Hua
机构信息
School of Chemistry and Chemical Engineering, Guangdong Pharmaceutical University, Guangzhou, 510006 (China), Fax: (+86) 760-88207939.
出版信息
Chem Asian J. 2014 Sep;9(9):2436-9. doi: 10.1002/asia.201402455. Epub 2014 Jul 2.
A general and efficient palladium-catalyzed direct C3 alkenylation of 4H-pyrido[1,2-a]pyrimidin-4-ones using AgOAc/O2 as the oxidant has been developed. A variety of 4H-pyrido[1,2-a]pyrimidin-4-ones were successfully coupled with acrylate esters, styrenes, methylvinylketone, and acrylamide in moderate to excellent yields. The reaction exhibited complete regio- and stereoselectivity. This transformation provides an attractive new approach to functionalize 4H-pyrido[1,2-a]pyrimidin-4-ones.
已开发出一种通用且高效的钯催化的4H-吡啶并[1,2-a]嘧啶-4-酮的直接C3烯基化反应，该反应使用醋酸银/氧气作为氧化剂。多种4H-吡啶并[1,2-a]嘧啶-4-酮成功地与丙烯酸酯、苯乙烯、甲基乙烯基酮和丙烯酰胺偶联，产率适中至优异。该反应表现出完全的区域选择性和立体选择性。这种转化为4H-吡啶并[1,2-a]嘧啶-4-酮的官能团化提供了一种有吸引力的新方法。
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