Copper‐Catalyzed Radical Silylarylation of Activated Alkenes: Preparation of β‐Silyl Amide‐Pharmaceutical Hybrids

Author:

Chen Fei1ORCID,Liu Shi‐Yu1,Li Xiao1,Jia Jia‐Lu1,Li Yi1,Lu Xiao‐Lan1,Jia Lin1,Zheng Yang1,Yan Zhongfei1,Li Gang1ORCID,Lv Yunhe1ORCID,Rong Haojie2

Affiliation:

1. Henan Province Key Laboratory of New Optoelectronic Functional Materials Henan Provincial Engineering and Technology Research Center for Precise Synthesis of Fluorine-Containing Drugs College of Chemistry and Chemical Engineering Anyang Normal University Anyang 455000 People's Republic of China

2. State Key Laboratory of Fluorine & Nitrogen Chemicals Modern Chemistry Research Institute of Xi'an Xi'an 710065 People's Republic of China

Abstract

AbstractCopper‐catalyzed silylarylation of N‐(arylsulfonyl)acrylamides via a tandem silyl radical addition/1,4‐aryl migration/desulfonylation sequence has been developed. This method employs silanes as the precursor of silyl radical and di‐tert‐butyl peroxide (DTBP) as the initiator. By using this cascade procedure, a series of β‐silyl amide‐pharmaceutical hybrids which contain an α‐all‐carbon quaternary stereocenter were facilely synthesized.

Funder

National Natural Science Foundation of China

Anyang Normal University

Publisher

Wiley

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