Jilin Province Key Laboratory of Organic Functional Molecular Design & Synthesis, Department of Chemistry, Northeast Normal University , Changchun 130024, China.
J Org Chem. 2017 Dec 1;82(23):12813-12820. doi: 10.1021/acs.joc.7b02148. Epub 2017 Nov 8.
A facile and efficient copper-catalyzed azidative multifunctionalization of alkynes has been developed by using N-fluorobenzenesulfonimide (NFSI) as both nitrogen source and aryl source and trimethylsilyl azide (TMSN) as azido source. This transformation proceeds under mild conditions, providing a series of α-azido-α-aryl imine in good yields by a single operation starting from a wide range of alkynes. The prepared α-azido-α-aryl imines could be easily converted into 1,5-piperizine-fused 1,2,3-triazoles and azido enamines.
一种简便高效的铜催化炔烃的叠氮化多官能化反应已经被开发出来,该反应以 N-氟代苯磺酰胺(NFSI)作为氮源和芳基源,三甲基硅叠氮(TMSN)作为叠氮源。该转化在温和条件下进行,通过从广泛的炔烃起始的单一操作,以良好的收率提供一系列α-叠氮-α-芳基亚胺。所制备的α-叠氮-α-芳基亚胺可以很容易地转化为 1,5-哌嗪并合的 1,2,3-三唑和叠氮烯胺。