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 

机构地区：[1]Department of Applied Chemistry,Anhui Province Engineering Laboratory for Green Pesticide Development and Application,and Anhui Province Key Laboratory of Crop Integrated Pest Management,Anhui Agricultural University,Hefei,Anhui 230036,China

出　　处：《Chinese Journal of Chemistry》2024年第18期2140-2146,共7页中国化学（英文版）

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.

摘　　要：Background and Originality Content,3,4-Dihydroquinazoline frameworks have frequently been encountered in natural products and bioactive molecules.In 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 design.For 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.

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

分 类 号：O62[理学—有机化学]