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

Copper‐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 p...

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Bibliographic Details
Published in:Advanced synthesis & catalysis 2024-03, Vol.366 (6), p.1325-1330
Main Authors: Chen, Fei, Liu, Shi‐Yu, Li, Xiao, Jia, Jia‐Lu, Li, Yi, Lu, Xiao‐Lan, Jia, Lin, Zheng, Yang, Yan, Zhongfei, Li, Gang, Lv, Yunhe, Rong, Haojie
Format: Article
Language:English
Subjects:
alkenes
Copper
copper-catalysis
late-stage modification of drug molecules
Pharmaceuticals
radical cascade reactions
silylarylation
β-silyl amides
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Summary:Copper‐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.
ISSN:1615-4150
1615-4169
DOI:10.1002/adsc.202301434