Boronic Acid → Methyl 3-cyclohexyl-2-(3-formyl-2-thienyl)1H-indole-6-carboxylate

Participants

Reaction Steps

Methyl 2-bromo-3-cyclohexyl1H-indole-6-carboxylate (prepared as described in published International patent application WO 2004/087714), (3-formyl-2-thienyl)boronic acid (1.2 eq), spray-dried KF (5 eq) and Pd(tBu3P)2 (0.2 eq) were dissolved in dioxane (0.15 M); the reaction mixture was stirred under N2 at RT for 4 h, then more KF, boronic acid and catalyst were added and stirring was continued overnight. All volatiles were evaporated in vacuo and the title compound was isolated by flash chromatography (PE/EtOAc 8:2). Yield 99%; MS (ES+) m/z 368 (M+H)+.

Provenance & Evidence