Pyrrole Functionalization by Copper‐Catalyzed Nitrene Transfer Reactions

The catalytic functionalization of pyrroles by incorporation of a nitrene group is reported. The Cα‐H bond of 1H‐pyrrole is amidated upon the formal insertion of the NTs (Ts=p‐toluenesulfonyl) group catalyzed by TpBr3Cu(NCMe) (TpBr3=hydrotris(3,4,5‐tribromo‐pyrazolyl)borate). N‐substituted pyrroles...

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Bibliographic Details
Authors: Moreno Rodríguez, Anabel, Ramírez Rodríguez, Manuel, Díaz Requejo, María Mar, Pérez Romero, Pedro José
Format: article
Publication Date:2020
Country:España
Institution:Universidad de Huelva (UHU)
Repository:Arias Montano. Repositorio Institucional de la Universidad de Huelva
Language:English
OAI Identifier:oai:ariasmontano.uhu.es:10272/19698
Online Access:http://hdl.handle.net/10272/19698
Access Level:Open access
Keyword:Nitrene transfer
Pyrrole functionalization
C-H amidation
Copper catalysis
Copper nitrene
23 Química
Description
Summary:The catalytic functionalization of pyrroles by incorporation of a nitrene group is reported. The Cα‐H bond of 1H‐pyrrole is amidated upon the formal insertion of the NTs (Ts=p‐toluenesulfonyl) group catalyzed by TpBr3Cu(NCMe) (TpBr3=hydrotris(3,4,5‐tribromo‐pyrazolyl)borate). N‐substituted pyrroles also verify the same transformation. The mechanism proposal is similar to that previously described for benzene amidation with the same catalyst and PhI=NTs, which takes place through aziridine formation, ring opening and 1,2‐hydrogen shift. A cascade reaction involving the coupling of 2,5‐dimethylfuran, 1,2,3‐trimethyl‐pyrrole and a nitrene NTs group is also described, leading to a 1,2‐dihydropyridine‐imine compound.