Hydrochloric Acid → 4'-Amino-2'-methyl-biphenyl-3-carboxylic acid (4-morpholin-4-yl-phenyl)-amide

Participants

Reaction Steps

[2-Methyl-3′-(4-morpholin-4-yl-phenylcarbamoyl)-biphenyl-4-yl]-carbamic acid tert-butyl ester (670 mg) was stirred in methanol (15 ml) and 5M HCl (5 ml) at 20 C for 2 days. TLC indicated that the reaction was progressing slowly and so the mixture was heated to reflux for 6 h. The reaction was allowed to cool and was then basified and extracted with dichloromethane. The dried extract was evaporated and the residue purified on silica gel. Elution with dichloromethane:ethanol:0.880 ammonia; 400:8:1 gave a colourless foam which crystallized on standing (354 mg).

Provenance & Evidence