反应详情

Add 1,8-diazabicyclo [5.4.0] undec-7-ene (DBU) drop wise (0.51 mL, 3.6 mmol) to a suspension of 6-amino-4′-[3-(propane-2-sulfonylamino)-thiophen-2-yl]-biphenyl-2-carboxylic acid methyl ester (208 mg 0.48 mmol) in dichloromethane (9 ml) at 0° C., followed by drop wise addition of isopropylsulfonyl chloride (0.21 mL, 0.9 mmol) and stir the reaction at room temperature overnight. Remove solvent under reduced pressure. Purify with flash chromatography (Silica gel-hexane/EtOAc). Concentrate the desired fractions to provide 6-(propane-2-sulfonylamino)-4′-[3-(propane-2-sulfonylamino)-thiophen-2-yl]-biphenyl-2-carboxylic acid methyl ester (50 mg). MS (m/e): 535.1(M−1).

1. customthe reaction at room temperature overnight
2. customPurify with flash chromatography (Silica gel-hexane/EtOAc)
3. concentrationConcentrate the desired fractions