1,2-Dichloroethane → HCID 57908098, compound

Participants

Reaction Steps

A solution of 2-aminobenzo[b]thiophene-3-carboxylic acid (1.0 g, 1.0 equivalent) and 4-piperidone (1.0 equivalent) in DMF (0.33 M) was treated with EDC (1.0 equivalent), HOBt (1.0 equivalent) and Et3N (2.0 equivalents) at rt. The reaction mixture was stirred until the reaction was complete as determined by LCMS analysis and then partitioned between ethyl acetate and water. Organic layers were washed with saturated aqueous NaHCO3 and brine, dried over Na2SO4, and volatiles removed under reduced pressure. Residue was purified by SiO2 chromatography (5%-10% MeOH/CH2Cl2 gradient) to afford the 1-(2-aminobenzo[b]thiophene-3-carbonyl)piperidin-4-one (6A, 84%).

Provenance & Evidence