Herein, we report an operationally simple, ligand- and additive-free oxidative boron-Heck coupling that is compatible with the ethenesulfonyl fluoride functional group. The protocol proceeds at room temperature with chemoselectivity and E-isomer selectivity and offers facile access to a wide range of β-aryl/heteroaryl ethenesulfonyl fluorides from commercial boronic acids. Furthermore, we demonstrate a "one-pot click" reaction to directly transform the products to aryl-substituted β-sultams.
C 9 H 13 FO5S, triclinic,
CCDC no.: 1528194The crystal structure is shown in the figure. Crystal data, data collection and structure refinement details are summarized in Tables 1. Tables 2 lists the
Source of materialA mixture of methyl 2-oxocyclopentane carboxylate (20 mg, 1.0 eq), thiourea (N,N-diisopropylethylamine; 0.20 eq) and DIPEA (0.20 eq) was stirred in toluene (1.0 mL) at room
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