Diisopropylethylamine → 1-(2-Chloro-6-morpholinopyrimidin-4-yl)piperidin-2-one

Participants

Reaction Steps

To a solution of HATU (304 mg, 0.8 mmol), HOAT (82 mg, 0.6 mmol) and DIEA (0.209 mL, 1.2 mmol) in chloroform (20 mL) under argon, a solution of 5-(2-chloro-6-morpholinopyrimidin-4-ylamino)pentanoic acid (190 mg, 0.6 mmol) in chloroform (10 mL) was slowly added. The reaction solution was stirred at room temperature for 5 hours. After the reaction was complete, the solution was evaporated to dryness to give a white solid which was chromatographed on a silica gel column by eluting with 40% EtOAc/hexane to give 1-(2-chloro-6-morpholinopyrimidin-4-yl)piperidin-2-one as a white solid (62 mg, 35%). LC/MS (m/z): 297.0 (MH+), Rt 2.74 minutes.

Provenance & Evidence