Regioselective C3 Alkenylation of 4 H‐pyrido[1,2‐a]pyrimidin‐4‐ones via Palladium‐Catalyzed CH Activation |
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| Authors: | Dr. Wenjie Liu Dr. Shaohua Wang Qi Zhang Jingwen Yu Jiahe Li Zhiwei Xie Prof. Hua Cao |
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| Affiliation: | School of Chemistry and Chemical Engineering, Guangdong Pharmaceutical University, Guangzhou, 510006 (China), Fax: (+86)?760‐88207939 |
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| Abstract: | 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. |
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| Keywords: | alkenylation C H activation homogeneous catalysis palladium regioselectivity |
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