De novo Synthesis of Chiral 3,4-Dihydroquinazolines via One-Pot Enantioselective Ugi-Azide/Cyclization Sequences

作     者：Zu-Kui Xie Jun-Jun Ding Yi-Ming Ou Jun-Xiu Shi Meng-Lan Shen Chuan-Zhi Yao Hua-Jie Jiang Jie Yu Zu-Kui Xie;Jun-Jun Ding;Yi-Ming Ou;Jun-Xiu Shi;Meng-Lan Shen;Chuan-Zhi Yao;Hua-Jie Jiang;Jie Yu

作者机构：Department of Applied ChemistryAnhui Province Engineering Laboratory for Green Pesticide Development and Applicationand Anhui Province Key Laboratory of Crop Integrated Pest ManagementAnhui Agricultural UniversityHefeiAnhui 230036China 

出 版 物：《Chinese Journal of Chemistry》 (中国化学（英文版）)

年 卷 期：2024年第42卷第18期

页      面：2140-2146页

核心收录：

学科分类：081704[工学-应用化学] 07[理学] 08[工学] 0817[工学-化学工程与技术] 070303[理学-有机化学] 0703[理学-化学] 

基　　金：financial support from NSFC(Grant No.92156022) Anhui Provincial Natural Science Funds(Grant Nos.2308085MB43,2308085QB44) Shennong Scholar Program of Anhui Agricultural University,and National Undergraduate Training Program for Innovation and Entrepreneurship 

主　　题：Anionic stereogenic-at-cobalt(ll)complex De novo synthesis post-Ugi transformation One-pot sequence Asymmetric synthesis Multicomponentreactions 

摘      要：Background and Originality Content,3,4-Dihydroquinazoline frameworks have frequently been encountered in natural products and bioactive *** the past decades,these key structures prompted the development of creative pharmaceuticals owing to their prominent biological properties,including trypanothione reductase(TryR)inhibitor,Hepatitis B virus(HBV)inhibitive activities,anticancer activities,etc.(Scheme 1A).[1]Notably,the chirality of the C4 atom is crucial for drug *** example,the DPC-083 is a potent reverse transcriptase inhibitor for the treatment of HIV infection but the undesired enantiomers exhibit virtually no activity.[ia]Therefore,developing synthetic methods for innovative chiral 4-substituted 3,4-dihydroquinazolines is significant and essential for drug discovery.