Benzoyl isothiocyanate → N-(((3S,4R,5S)-3-(2,3-difluorophenyl)-4-(hydroxymethyl)-5-((trityloxy)methyl)tetrahydrofuran-3-yl)carbamothioyl)benzamide

Participants

Reaction Steps

Benzoyl isothiocyanate (2.1 ml) was added to a solution of [(2S,3R,4S)-4-amino-4-(2,3-difluorophenyl)-2-((trityloxy)methyl)tetrahydrofuran-3-yl]methanol, obtained in Preparation Example 4-(23), (7.04 g) in DCM (26 ml) at 0° C. After stirring for 10 h and 50 mins at same temperature, the mixture was directly purified by silica gel column chromatography (gradient from 20% to 50% EtOAc in heptane) to afford the titled compound (9.47 g) as a pale yellow solid.

Provenance & Evidence