Phenyl thioxochloroformate → thiocarbonic acid O-[(4-cyano-3-fluoro-phenyl)-pyridin-3-yl-methyl]Ester O-phenyl Ester

Participants

Reaction Conditions

Reaction Steps

To a solution of 2-fluoro-4-(hydroxy-pyridin-3-yl-methyl)-benzonitrile (as described in Example 20, Step C) (0.4 g, 1.75 mmol) in CH2Cl2 (25.0 mL) at 0° C. was added phenyl thionochloroformate (0.388 mL, 2.8 mmol) and DMAP (0.471 g, 3.86 mmol). The solution was stirred at 25° C. for 3 hr. The reaction was partitioned with saturated NaHCO3 and CH2Cl2. The CH2Cl2 layer was washed with brine, dried with MgSO4, and evaporated in vacuo to obtain the title compound after chromatography (silica gel, CH2Cl2:MeOH 99:1).

Provenance & Evidence