反应详情

Benzoyl isothiocyanate (0.6 g, 3.7 mmol) was added drop-wise to a solution of rel-[(2S,4R,5S)-5-amino-2-(cyclopropylmethyl)-5-(2,4-difluorophenyl)tetrahydro-2H-pyran-4-yl]methanol (C71) (1.10 g, 3.7 mmol) in dichloromethane (30 mL). After the reaction mixture had stirred at room temperature for 15 hours, it was concentrated in vacuo. Purification via silica gel chromatography (Gradient: 0% to 20% ethyl acetate in petroleum ether) provided the product as a brown solid. Yield: 1.14 g, 2.47 mmol, 67%. LCMS m/z 461 [M+H+].

1. concentrationit was concentrated in vacuo
2. customPurification via silica gel chromatography (Gradient: 0% to 20% ethyl acetate in petroleum ether)