3-Fluoropyridine-4-boronic acid hydrate → 5-Fluoro-3-methyl-benzo[b]thiophene-2-sulfonic acid [4-(3-fluoro-pyridin-4-yl)-2-trifluoromethyl-phenyl]-amide

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Reaction Steps

This compound was prepared in analogy to Example 2 starting from 5-fluoro-3-methyl-benzo[b]thiophene-2-sulfonic acid(4-bromo-2-trifluoromethyl-phenyl)-amide (0.12 g) and 3-fluoropyridine-4-boronic acid hydrate (0.061 g) in 1,2-dimethoxyethane (1.5 ml), ethanol (0.32 ml) and 2 M aqueous sodium carbonate solution (1.0 ml) with tetrakis(triphenylphosphine)palladium (0.050 g) to obtain the title compound (0.025 g) as a yellowish foam. MS (ISP): 485.3 (M+H)+

Provenance & Evidence