文献类型：期刊文献

英文题名：Ti-Catalyzed Formal [2π+2σ] Cycloadditions of Bicyclo[1.1.0]butanes with 2-Azadienes to Access Aminobicyclo[2.1.1]hexanes

作者：Ren, Haosong[1];Li, Tianxiang[1];Xing, Jinping[1];Li, Zhenyue[1];Zhang, Yanxia[2];Yu, Xinhong[1];Zheng, Jun[1]

机构：[1]East China Univ Sci & Technol, Engn Res Ctr Pharmaceut Proc Chem, Sch Pharm, Minist Educ, Shanghai 200237, Peoples R China;[2]Chinese Acad Sci, Shanghai Inst Organ Chem, State Key Lab Organometall Chem, Shanghai 200032, Peoples R China

年份：2024

卷号：26

期号：8

起止页码：1745

外文期刊名：ORGANIC LETTERS

收录：;WOS:【SCI-EXPANDED(收录号:WOS:001173670200001)，CCR-EXPANDED(收录号:WOS:001173670200001)】；

基金：We are grateful for the financial support from the National Natural Science Foundation of China (22301075), Shanghai Scientific and Technological Innovation Projects (23ZR1417400), East China University of Science and Technology for startup funding, the Program of Introducing Talents of Discipline to Universities, and the 111 Project (BP0719034). The authors thank the Research Center of Analysis and Test of East China University of Science and Technology for the help on NMR analysis.

语种：英文

摘要：Saturated bicyclic amines are increasingly targeted to the pharmaceutical industry as sp3-rich bioisosteres of anilines. Numerous strategies have been established for the preparation of bridgehead aminobicyclics. However, methods to assemble the bridge-amino hydrocarbon skeleton, which serves as a meta-substituted arene bioisostere, are limited. Herein, a general approach to access 2-aminobicyclo[2.1.1]hexanes (aminoBCHs) by titanium-catalyzed formal [2 pi + 2 sigma] cycloaddition of bicyclo[1.1.0]butanes and 2-azadienes was developed. Simple derivatization of aminoBCHs leads to various medicinally and agrochemically important analogues.