2-Aminothiazole → HCID 57901677, compound

Participants

Reaction Conditions

Reaction Steps

A mixture of 7-[(2-thienylsulfonyl)amino]-1H-indole-2-carboxylic acid (200 mg), 2-aminothiazole (75 mg), ethyldiisopropylamine (0.16 mL), 0-(7-azabenzotriazol-1-yl)-N,N,N′,N′-tetramethyluronium hexafluorophosphate (354 mg) and N,N-dimethylformamide (8 mL) was stirred at 60° C. for 18 hr. The reaction mixture was diluted with ethyl acetate, washed with aqueous citric acid solution, aqueous sodium hydrogencarbonate solution and saturated brine, dried over anhydrous magnesium sulfate, and concentrated under reduced pressure. The obtained residue was subjected to silica gel column chromatography (ethyl acetate), and the obtained crystals were washed with ethyl acetate-hexane to give the title compound (197 mg, yield 78%) as pale-yellow crystals. melting point 300-302° C. (decomposition).

Provenance & Evidence