Construction of α-(Hetero)aryl Ethenesulfonyl Fluorides for SuFEx Click Chemistry

Abstract

The construction of α-(hetero)aryl ethenesulfonyl fluorides was achieved via a Pd-catalyzed Suzuki coupling of arylboronic acids with 1-bromoethene-1-sulfonyl fluoride (1-Br-ESF). The novel α-aryl ethenesulfonyl fluorides were found to be another selectively addressable bis-electrophile for wide diversification through SuFEx click chemistry, or Michael addition with excellent chemical discrimination.