Institute of Drug Discovery and Design, College of Pharmaceutical Sciences, Zhejiang University, 866 Yuhangtang road, Hangzhou, 310058, China.
Angew Chem Int Ed Engl. 2022 Jul 11;61(28):e202205037. doi: 10.1002/anie.202205037. Epub 2022 May 17.
The cycloaddition of azides and alkynes is the leading click chemistry technology and has been widely used in drug discovery, biology and material sciences. However, the development of a modular and scalable enantioselective click cycloaddition remains a long-standing challenge. Herein, we report a rhodium-catalyzed enantioselective click cycloaddition of azides and alkynes for rapid and modular access to atropisomeric triazoles in excellent yields and enantioselectivities. The process is mild, efficient and scalable, and features broad substrate scope.
叠氮化物和炔烃的环加成是主要的点击化学技术，已广泛应用于药物发现、生物学和材料科学。然而，开发模块化和可扩展的对映选择性点击环加成仍然是一个长期存在的挑战。在此，我们报告了一种铑催化的对映选择性点击环加成反应，可快速、模块化地获得具有优秀产率和对映选择性的轴手性三唑。该过程温和、高效且可扩展，具有广泛的底物范围。
