6274-53-9Relevant articles and documents
Direct β- and γ-C(sp3)?H Alkynylation of Free Carboxylic Acids**
Ghiringhelli, Francesca,Ghosh, Kiron Kumar,Uttry, Alexander,van Gemmeren, Manuel
supporting information, p. 23127 - 23131 (2020/10/15)
In this study we report the identification of a novel class of ligands for palladium-catalyzed C(sp3)?H activation that enables the direct alkynylation of free carboxylic acid substrates. In contrast to previous synthetic methods, no introduction/removal of an exogenous directing group is required. A broad scope of acids including both α-quaternary and challenging α-non-quaternary can be used as substrates. Additionally, the alkynylation in the distal γ-position is reported. Finally, this study encompasses preliminary findings on an enantioselective variant of the title transformation as well as synthetic applications of the products obtained.