[CH2:1]([O:8][C:9]1[C:14]2[C:15]([O:18][CH2:19][CH2:20][CH:21]3[CH2:26][CH2:25][NH:24][CH2:23][CH2:22]3)=[N:16][O:17][C:13]=2[CH:12]=[CH:11][CH:10]=1)[C:2]1[CH:7]=[CH:6][CH:5]=[CH:4][CH:3]=1.[C:27](=O)([O-])[O-].[K+].[K+].C=O.[CH2:35]([OH:37])[CH3:36]>>[CH2:1]([O:8][C:9]1[C:14]2[C:15]([O:18][CH2:19][CH2:20][CH:21]3[CH2:26][CH2:25][N:24]([CH2:27][O:37][CH2:35][CH3:36])[CH2:23][CH2:22]3)=[N:16][O:17][C:13]=2[CH:12]=[CH:11][CH:10]=1)[C:2]1[CH:3]=[CH:4][CH:5]=[CH:6][CH:7]=1To a stirred mixture of 4-(benzyloxy)-3-(2-piperidin-4-ylethoxy)-1,2-benzisoxazole (3.1 g, 8.4 mmol, EXAMPLE 7, Step 3) and potassium carbonate (1.2 g, 8.4 mmol) in ethanol (16.0 mL) was added paraformaldehyde (0.28 g, 9.2 mmol) at ambient temperature. After being stirred at room temperature for 14 h, the mixture was filtered. The filtrate was concentrated in vacuo to give 3.4 g (quant.) of the title compound as a colorless oil.
Wird geladen…