Metal-Free C-2-H Alkylation of Quinazolin-4-ones with Alkanes via Cross-Dehydrogenative Coupling. 2019

Shuai Mao, and Kaixiu Luo, and Lu Wang, and Hong-Yi Zhao, and Andrea Shergalis, and Minhang Xin, and Nouri Neamati, and Yi Jin, and San-Qi Zhang
Department of Medicinal Chemistry, School of Pharmacy , Xi'an Jiaotong University , Xi'an 710061 , China.

A practically useful approach for the cross-dehydrogenative coupling of quinazolin-4-one with simple nonactivated alkanes is reported. The products were smoothly formed under mild reaction conditions, within short reaction time at ambient temperature. The formation of new Csp3-Csp2 bonds occurred at the electron-poor C-2 position of quinazolin-4-one. The approach has the potential to be an important tool for the late-stage functionalization of advanced synthetic intermediates and may find many applications in medicinal chemistry.

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