Methyl 2-(3-aminophenoxy)acetate → 3-{[6-(4-Bromophenyl)-5-(4-fluorophenyl)furo[2,3-d]pyrimidin-4-yl]amino}phenoxyacetic acid methyl ester

Participants

Reaction Steps

Heat 400 mg (0.991 mmol) of 6-(4-bromophenyl)-4-chloro-5-(4-fluorophenyl)furo[2,3-d]pyrimidine (for preparation see WO 03/018589) and 215.5 mg (1.19 mmol) of 3-aminophenoxyacetic acid methyl ester to 150° C. in an oil bath for 1.5 h. After cooling, take up the residue in DMSO and filter through silica gel (eluent: dichloromethane/ethyl acetate 10:1). 242 mg of a mixture are isolated, which is purified by preparative HPLC. 120 mg (15% of theory) of the target compound are obtained as a colourless solid.

Provenance & Evidence