State Key Laboratory of Applied Organic Chemistry, Lanzhou University , Lanzhou 730000, China.
J Org Chem. 2017 Aug 18;82(16):8761-8768. doi: 10.1021/acs.joc.7b01497. Epub 2017 Aug 8.
A copper-catalyzed oxidative cyclization procedure has been developed for the production of 2-sulfonated 9H-pyrrolo[1,2-a]indol-9-ones via the direct sulfonylation of N-propargyl-substituted indoles with sulfonylhydrazides and tert-butyl hydroperoxide (TBHP). This novel protocol, which tolerates a broad range of functional groups, offers a simple, efficient, and atom-economical route to a series of fluorazones in good yields under mild conditions.
一种铜催化的氧化环化方法已经被开发出来,用于通过 N-丙炔基取代的吲哚与磺酰基腙和叔丁基过氧化氢(TBHP)的直接磺酰化反应来制备 2-磺酰基 9H-吡咯并[1,2-a]吲哚-9-酮。该新方法可以容忍广泛的官能团,在温和条件下以良好的收率提供了一种简单、高效和原子经济性的方法来合成一系列氟唑酮。