Propylphosphonic anhydride → HCID 178451399、化合物

反応式

[NH2:1][CH:2]1[CH2:8][CH:7]2[N:9]([C:10]([O:12][C:13]([CH3:16])([CH3:15])[CH3:14])=[O:11])[CH:4]([CH2:5][CH2:6]2)[CH2:3]1.[NH:17]1[CH:21]=[C:20]([CH2:22][CH2:23][CH2:24][C:25](O)=[O:26])[N:19]=[N:18]1.C(P1(=O)OP(CCC)(=O)OP(CCC)(=O)O1)CC>CN(C=O)C>[NH:17]1[CH:21]=[C:20]([CH2:22][CH2:23][CH2:24][C:25]([NH:1][CH:2]2[CH2:3][CH:4]3[N:9]([C:10]([O:12][C:13]([CH3:16])([CH3:15])[CH3:14])=[O:11])[CH:7]([CH2:6][CH2:5]3)[CH2:8]2)=[O:26])[N:19]=[N:18]1

参加物

実験手順

A reaction mixture comprising of tert-butyl 3-amino-8-azabicyclo[3.2.1]octane-8-carboxylate (250 mg, 1.105 mmol), 4-(1H-1,2,3-triazol-4-yl)butanoic acid (Example 17, step 4) (171 mg, 1.105 mmol), T3P® 50% DMF (1.29 ml, 2.209 mmol) and TEA (462 μl, 3.31 mmol) in DMF (3.6 ml) was stirred for 4 hours. The reaction mixture was concentrated under reduced pressure. The resulting oil was diluted with DCM and washed with water. The organic portion was dried over MgSO4, filtered and concentrated under reduced pressure. The material was taken crude to the next step.