Polycyclic Indoline-Benzodiazepines through Electrophilic Additions of α-Imino Carbenes to Tröger Bases

通过α-亚氨基卡宾对Tröger碱的亲电加成反应合成多环吲哚啉-苯二氮杂卓

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Abstract

Polycyclic indoline-benzodiazepines can be accessed through the intermolecular reaction of Tröger bases with N-sulfonyl-1,2,3-triazoles. Under Rh(II) catalysis, α-imino carbenes are generated and a subsequent cascade of [1,2]-Stevens, Friedel-Crafts, Grob, and aminal formation reactions yield the polycyclic heterocycles as single isomers (d.r.>49:1, four stereocenters including two bridgehead N atoms). Further ring expansion by insertion of a second α-imino carbene leads to elaborated polycyclic 9-membered-ring triazonanes.

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