Morpholine → HCID 86706367、化合物

反応式

[CH:1]1([CH2:6][C@H:7]([CH2:32][N:33]([CH:41]=[O:42])[O:34][CH:35]2[CH2:40][CH2:39][CH2:38][CH2:37][O:36]2)[C:8]([N:10]2[CH:14]([C:15]([NH:17][C:18]3[N:23]=[CH:22][C:21]([O:24][CH3:25])=[CH:20][N:19]=3)=[O:16])[CH2:13][CH2:12][N:11]2C(OCC=C)=O)=[O:9])[CH2:5][CH2:4][CH2:3][CH2:2]1.N1CCOCC1>ClCCl.C1C=CC([P]([Pd]([P](C2C=CC=CC=2)(C2C=CC=CC=2)C2C=CC=CC=2)([P](C2C=CC=CC=2)(C2C=CC=CC=2)C2C=CC=CC=2)[P](C2C=CC=CC=2)(C2C=CC=CC=2)C2C=CC=CC=2)(C2C=CC=CC=2)C2C=CC=CC=2)=CC=1>[CH:1]1([CH2:6][C@H:7]([CH2:32][N:33]([CH:41]=[O:42])[O:34][CH:35]2[CH2:40][CH2:39][CH2:38][CH2:37][O:36]2)[C:8]([N:10]2[C@H:14]([C:15]([NH:17][C:18]3[N:23]=[CH:22][C:21]([O:24][CH3:25])=[CH:20][N:19]=3)=[O:16])[CH2:13][CH2:12][NH:11]2)=[O:9])[CH2:2][CH2:3][CH2:4][CH2:5]1

参加物

実験手順

Pd(Ph3P)4 (23.77 mg, 0.021 mmol) 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-({[5-(methyloxy)-2-pyrimidinyl]amino}carbonyl)-1-pyrazolidinecarboxylate (173 mg, 0.294 mmol) and morpholine (81 μl, 0.935 mmol) in dichloromethane (DCM) (4.1 ml). The mixture was stirred at ambient temperature for 30 min. The solvent was removed under reduced pressure to give a crude product which was purified by RP-HPLC to give (3S)-2-((2R)-3-cyclopentyl-2-{[formyl(tetrahydro-2H-pyran-2-yloxy)amino]methyl}propanoyl)-N-[5-(methyloxy)-2-pyrimidinyl]-3-pyrazolidine carboxamide (67 mg, 0.133 mmol, 45% yield). MS (ES+) m/z 505.2 (MH+).