1-((Tert-butoxy)carbonyl)-3,3-dimethylpyrrolidine-2-carboxylic acid → 1-(tert-butoxycarbonyl)-3,3-dimethylprolyl-N-[5-chloro-2-(1H-tetraazol-yl)-benzyl]-L-prolinamide
反応式
[C:1]([O:5][C:6]([N:8]1[CH2:15][CH2:14][C:13]([CH3:17])([CH3:16])[CH:9]1[C:10]([OH:12])=O)=[O:7])([CH3:4])([CH3:3])[CH3:2].[Cl:18][C:19]1[CH:20]=[CH:21][C:22]([N:34]2[CH:38]=[N:37][N:36]=[N:35]2)=[C:23]([CH:33]=1)[CH2:24][NH:25][C:26](=[O:32])[C@@H:27]1[CH2:31][CH2:30][CH2:29][NH:28]1>C(Cl)CCl>[C:1]([O:5][C:6]([N:8]1[CH2:15][CH2:14][C:13]([CH3:17])([CH3:16])[C@H:9]1[C:10]([N:28]1[CH2:29][CH2:30][CH2:31][C@H:27]1[C:26]([NH:25][CH2:24][C:23]1[CH:33]=[C:19]([Cl:18])[CH:20]=[CH:21][C:22]=1[N:34]1[CH:38]=[N:37][N:36]=[N:35]1)=[O:32])=[O:12])=[O:7])([CH3:2])([CH3:3])[CH3:4]参加物
4
反応物 2
生成物 1
試薬・触媒・溶媒 1
実験手順
The title compound was prepared as a mixture of diastereomers from 1-(tert-butoxycarbonyl)-3,3-dimethyl-dl-proline (61 mg, 0.25 mmol) and N-[5-chloro-2-(1H-tetrazol-1-yl)benzyl]-L-prolinamide (Example 26, Step B, 95 mg, 0.25 mmol) essentially according to the EDC coupling procedure described in Example 39, Step D. The diastereomeric products were separated by reverse phase HPLC and were carried on directly to deprotection.