Synthesis of α,α-Difluoromethylene Alkynes by Palladium-Catalyzedgem-Difluoropropargylation of Aryl and Alkenyl Boron Reagents

Autor: Yanbo Yu, Xingang Zhang, Guo-Zhen He
Rok vydání: 2014
Předmět:
Zdroj: Angewandte Chemie. 126:10625-10629
ISSN: 0044-8249
DOI: 10.1002/ange.201405204
Popis: gem-Difluoropropargyl bromides are versatile intermediates in organic synthesis, but have rarely been employed in transition-metal-catalyzed cross-coupling reactions. The first palladium-catalyzed gem-difluoropropargylation of organoboron reagents with gem-difluoropropargyl bromides is now reported. The reaction proceeds under mild reaction conditions with high regioselectivity; it features a broad substrate scope and excellent functional-group compatibility and thus provides an attractive approach for the synthesis of complex fluorinated molecules, in particular for drug discovery and development.
Databáze: OpenAIRE