title: Regioselective C3 alkenylation of 4 H-pyrido[1,2-a]pyrimidin-4-ones via palladium-catalyzed C-H activation.
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.
authors.affiliation: School of Chemistry and Chemical Engineering, Guangdong Pharmaceutical University, Guangzhou, 510006 (China), Fax: (+86) 760-88207939.
authors.forename: Wenjie
authors.initials: W
authors.lastname: Liu
authors.forename: Shaohua
authors.initials: S
authors.lastname: Wang
authors.forename: Qi
authors.initials: Q
authors.lastname: Zhang
authors.forename: Jingwen
authors.initials: J
authors.lastname: Yu
authors.forename: Jiahe
authors.initials: J
authors.lastname: Li
authors.forename: Zhiwei
authors.initials: Z
authors.lastname: Xie
authors.forename: Hua
authors.initials: H
authors.lastname: Cao
mesh_terms: D000478:Alkylation; D002384:Catalysis; D015394:Molecular Structure; D009942:Organometallic Compounds / Q000737:chemistry*; D010165:Palladium / Q000737:chemistry*; D011725:Pyridines / Q000737:chemistry*; D011744:Pyrimidinones / Q000737:chemistry*; D013237:Stereoisomerism
chemical_list: D009942:Organometallic Compounds; D011725:Pyridines; D011744:Pyrimidinones; D010165:Palladium
keywords: CH activation; alkenylation; homogeneous catalysis; palladium; regioselectivity