Morpholine → HCID 86706361, compound

Participants

Reaction Steps

Pd(Ph3P)4 (4.63 mg, 4.01 μmol) was added to a solution of 2-propen-1-yl 2-((2R)-3-cyclopentyl-2-{[formyl(tetrahydro-2H-pyran-2-yloxy)amino]methyl}propanoyl)-3-[(2-pyrimidinylamino)carbonyl]-1-pyrazolidinecarboxylate (32 mg, 0.057 mmol) and morpholine (15.87 μl, 0.182 mmol) in dichloromethane (DCM) (0.8 ml). The mixture was stirred at ambient temperature for 15 min. The solvent was removed to give a residue which was purified by RP-HPLC to give (3S)-2-((2R)-3-cyclopentyl-2-{[formyl(tetrahydro-2H-pyran-2-yloxy)amino]methyl}propanoyl)-N-2-pyrimidinyl-3-pyrazolidinecarboxamide (13 mg, 0.027 mmol, 60% yield). MS (ES+) m/z 475.1 (MH+).

Provenance & Evidence