Formic Acid → 6-(2-Fluorophenyl)-5-(4-methoxyphenyl)-4-[(3R)-piperidin-3-yloxy]furo[2,3-d]pyrimidine formate

Participants

Reaction Steps

Add 400 mg of palladium black to an argon-blanketed solution of 510 mg (1.00 mmol) of 4-{[(3R)-1-benzylpiperidin-3-yl]oxy}-6-(2-fluorophenyl)-5-(4-methoxyphenyl)furo[2,3-d]pyrimidine in 5 ml of a 4.4% solution of formic acid in methanol, and stir at room temperature for two days. After filtering off the catalyst, wash the catalyst residue with methanol/water. Concentrate the filtrate under reduced pressure and purify the residue by means of preparative RP-HPLC (eluent: water/acetonitrile gradient with 0.1% formic acid). 70 mg (12% of theory, 80% purity) of the desired product are obtained.

Provenance & Evidence