Water → HCID 57703747, compound

Participants

Reaction Conditions

Reaction Steps

A mixture of (3′-Chloro-2-fluoro-6-methoxy-biphenyl-3-yl)-acetic acid (I-79) (0.998 mmol, 1.0 eq.) and thiosemicarbazide (2.99 mmol; 3 eq.) in excess phosphorous oxychloride was heated to 120° C. for 45 minutes, and allowed to cool to room temperature. The resultant mixture was added to water, and extracted with 2 portions of ethyl acetate. The organics were washed with brine, and dried over magnesium sulfate. The residue was purified via flash chromatography on silica gel using 5% (1N NH3 in MeOH) in dichloromethane as eluent to afford the desired product (P-333) in 39% yield.

Provenance & Evidence