Methanol → 5-[5-(4-Methoxy-phenyl)-pyrimidin-2-ylamino]-2-methyl-nicotinic acid

Participants

Reaction Steps

To a suspension of the 5-[5-(4-methoxy-phenyl)-pyrimidin-2-ylamino]-2-methyl-nicotinic acid ethyl ester 9 (0.9 mmol) in THF:MeOH:H2O=3:2:1 (7 mL), is added 6M LiOH (2.7 mmol). The reaction mixture is stirred at rt for 12 h. After this time the solvent is removed under vacuum, the residue is diluted with H2O (6 mL) and the pH neutralized with 6M HCl. The solid formed is filtered, washed with water and dried in a vacuum oven for 12 h to afford 5-[5-(4-methoxy-phenyl)-pyrimidin-2-ylamino]-2-methyl-nicotinic acid 10 as off white solid, which is used in the next step without further purification. MS (m/z) (M+1)+: 337.2.

Provenance & Evidence