【论文发表】Metal-Free C-2-H Alkylation of Quinazolin-4-ones with Alkanes via Cross-Dehydrogenative Coupling
Shuai Mao†§⊥, Kaixiu Luo‡⊥, Lu Wang†, Hong-Yi Zhao†, Andrea Shergalis§, Minhang Xin†, Nouri Neamati*§, Yi Jin*‡, and San-Qi Zhang*†
†Department of Medicinal Chemistry, School of Pharmacy, Xi’an Jiaotong University , Xi’an 710061 ,China
‡Key Laboratory of Medicinal Chemistry for Natural Resource, Ministry of Education and Yunnan Province, School of Chemical Science and Technology, Yunnan University , Kunming 650091 ,P. R. China
§Department of Medicinal Chemistry, College of Pharmacy,University of Michigan, Ann Arbor , Michigan 48109,United States
Org. Lett. 2019, 21, 7, 2365-2368
Publication Date (Web): March 25, 2019
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-Csp2bonds occurred at the electron-poor C-2 position ofquinazolin-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.