1,2-Dichloroethane → 7-[(3R)-3-[(1,1-Dimethylethoxycarbonyl)amino]-4-(2,5-difluorophenyl)butanoyl]-2-(ethylthio)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine

Participants

Reaction Steps

A mixture of 47 mg (0.19 mmol) of 2-(ethylthio)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine hydrochloride, 59 mg (0.19 mmol) of (3R)-3-[(1,1-dimethylethoxycarbonyl)amino]-4-(2,5-difluorophenyl)butanoic acid, 37 mg (0.19 mmol) of EDC, 26 mg (0.19 mmol) of HOBt, and 0.15 mL (0.57 mmol) of diisopropylethylamine in 1.5 mL of dichloromethane was stirred at ambient temperature overnight. The mixture was subjected directly to purification by flash chromatography (5 g silica gel cartridge, 20-to-50% ethyl acetate/hexane step gradient) to give 85 mg (91%) of the title compound as a white solid.

Provenance & Evidence