Abstract

Abstract Alkynylation reaction of 2,2-difluoro-1-iodoethenyl p-toluenesulfonate 1 with alkynyltributylstannanes in the presence of 10 mol% Pd(PPh3)4 and 10 mol% CuI in THF at reflux temperature for 3 h provided the corresponding 1,1-difluoro-1,3-enynyl tosylates 2 in 65–85% yields. The further arylation reaction of 2 with aryltributylstannanes in the presence of 10 mol% Pd(PPh3)2Cl2 and 3 equiv. of LiBr in THF at reflux temperature for 8 h afforded the coupled products 3 in 32–83% yields.

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