反应详情

To a mixture of 3-(2-{7-[methyl(2-thienylsulfonyl)amino]-1H-indol-2-yl}-1,3-thiazol-5-yl)propanoic acid (0.30 g), 1H-1,2,3-benzotriazol-1-ol (0.11 g) and N,N-dimethylformamide (8 mL) was added N-[3-(dimethylamino)propyl]-N′-ethylcarbodiimide hydrochloride (0.15 g) at room temperature. The mixture was stirred at room temperature for 2 hr, and morpholine (0.30 g) was added. The reaction mixture was stirred at room temperature overnight, and water was added. The resulting crystals were collected by filtration and dried. The obtained crystals were subjected to silica gel column chromatography and the title compound (0.24 g, yield 69%) was obtained as yellow crystals from a fraction eluted with tetrahydrofuran-hexane (2:1, volume ratio). The crystals were recrystallized from ethyl acetate-hexane. melting point 160-161° C.

1. stirringThe reaction mixture was stirred at room temperature overnight
2. filtrationThe resulting crystals were collected by filtration
3. customdried