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Title: Palladium-Catalyzed Direct α-Arylation of p-Methoxybenzyl-Protected S,S-Dimethylsulfoximine      
dateReleased:
02-16-2017
privacy:
information not avaiable
aggregation:
instance of dataset
dateCreated:
10-12-2016
refinement:
curated
ID:
doi:10.4125/PD0084TH
creators:
Sirvent, Juan
Bierer, Donald
Webster, Robert
Lücking, Ulrich
availability:
available
types:
other
description:
Sulfoximines have recently gained considerable recognition as an important structural motif in the life sciences. This is especially true for (hetero)aryl-substituted S,S-dimethylsulfoximine derivatives, such as the marketed insecticide sulfoxaflor, as well as the clinical candidates­ PTEFb inhibitor BAY 1143572 and ATR inhibitor AZD 6738 for the treatment of cancer. Herein, the first palladium-catalyzed direct α-arylation of p-methoxybenzyl-protected S,S-dimethylsulfoximine using readily available (hetero)aryl bromides is reported. This new method provides a safe, short, and efficient approach to (hetero)aryl-substituted­ S,S-dimethylsulfoximine derivatives, an important class of bioactive compounds, demonstrated by application of this methodology to an improved synthesis of PTEFb inhibitor BAY 1143572.
accessURL: https://doi.org/10.4125/PD0084TH
storedIn:
© Georg Thieme Verlag
qualifier:
not compressed
format:
HTML
accessType:
landing page
authentication:
none
authorization:
none
abbreviation:
Thieme Chemistry
homePage: https://www.thieme.de/
ID:
SCR:SCR_014699
name:
Thieme Chemistry

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