Pivalic acid → HCID 67208614, compound

Participants

Reaction Conditions

Reaction Steps

A 5 mL vial was charged with 3-(2-cyclohexyl-6-oxo-piperidin-1-yl)-thiophene-2-carboxylic acid methyl ester (32 mg, 0.10 mmol, 1.0 equiv), 1-bromo-4-fluoro benzene (17 mg, 0.10 mmol, 1.0 equiv), potassium carbonate (20.6 mg, 0.15 mmol, 1.5 equiv), tricyclophenylphosphine tetrafluoroborate (8.7 mg, 0.024 mmol, 0.24 equiv), Pd(OAc)2 (2.7 mg, 0.012 mmol, 0.12 equiv), pivalic acid (6.1 mg, 0.060 mmol, 0.6 equiv) and DMA (0.3 mL). The resulted mixture was flushed with nitrogen and stirred at 100° C. for 18 hours. The mixture was loaded to silica gel column and flushed with EtOAc/heptane 67% to give product 27 mg (yield 65%).

Provenance & Evidence