Toluene → 3-[5-(4-Fluorophenylcarbamoyl)pyrimidin-2-ylamino]-propionic acid

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Reaction Steps

A solution of 3-[5-(4-fluorophenylcarbamoyl)pyrimidin-2-ylamino]propionic acid tert-butyl ester in 90% trifluoroacetic acid/water was stirred for 15 min. Toluene (4 mL) was added and the solution was concentrated in vacuo. A series of dilutions and concentrations were performed using acetic acid/toluene (1/1) followed by methanol/toluene (1/1). The resulting solids were triturated with ethyl acetate/hexane (2/1) to afford 61.1 mg (98% yield) of the titled product as a white solid. API-MS m/z 305 (MH)+, 303 (M−H)−.

Provenance & Evidence