p-Toluenesulfonic acid → HCID 66744002, compound

Participants

Reaction Steps

A mixture of 3-amino-5-(pyridin-4-yl)thiophene-2-carboxamide (110 mg, 0.502 mmol), 1,1,1-trifluoroacetone (1 mL, 11.2 mmol), PTSA (9.5 mg, 0.050 mmol), MgSO4 (60.4 mg, 0.50 mmol) and DMF (1 mL) was microwave-irradiated at 100° C. for 1 h then at 130° C. for 3 h. Then, the mixture was poured into saturated aqueous NaHCO3 (100 mL). Extraction with EtOAc (100 mL), washing with brine, drying over MgSO4, filtration and concentration under reduced pressure gave a yellow solid. This residue was purified by column chromatography (Purif, NH, hexane to EtOAc) to afford a yellow solid. This solid was triturated with EtOAc/hexane and collected by filtration to afford the title compound (94.3 mg, 60%) as a yellow solid:

Provenance & Evidence