Hydrochloric Acid → (R)-5-ethyl-6-(1-methyl-2-(pyrrolidin-2-yl)-1H-indol-5-yl)-2-oxo-1,2-dihydropyridine-3-carboxylic acid
反応式
C(OC([N:8]1[CH2:12][CH2:11][CH2:10][C@@H:9]1[C:13]1[N:14]([CH3:36])[C:15]2[C:20]([CH:21]=1)=[CH:19][C:18]([C:22]1[C:31]([CH2:32][CH3:33])=[CH:30][C:25]([C:26]([O:28]C)=[O:27])=[C:24]([O:34]C)[N:23]=1)=[CH:17][CH:16]=2)=O)(C)(C)C.Cl>>[CH2:32]([C:31]1[CH:30]=[C:25]([C:26]([OH:28])=[O:27])[C:24](=[O:34])[NH:23][C:22]=1[C:18]1[CH:19]=[C:20]2[C:15](=[CH:16][CH:17]=1)[N:14]([CH3:36])[C:13]([C@H:9]1[CH2:10][CH2:11][CH2:12][NH:8]1)=[CH:21]2)[CH3:33]参加物
3
実験手順
(R)-Methyl 6-(2-(1-(tert-butoxycarbonyl)pyrrolidin-2-yl)-1-methyl-1H-indol-5-yl)-5-ethyl-2-methoxynicotinate (0.190 g, 0.38 mmol) was heated with 6M HCl (2.0 mL) at 80° C. for 2.5 h until complete conversion to the product was observed by LC/MS. HCl was removed under reduced pressure, residue triturated with Et2O and solid was collected by filtration. (R)-5-ethyl-6-(1-methyl-2-(pyrrolidin-2-yl)-1H-indol-5-yl)-2-oxo-1,2-dihydropyridine-3-carboxylic acid (0.149 g, 96%) was obtained as yellow solid.