4-Amino-5-chloro-2-methoxybenzoic acid → 2,3-methylenedioxy-N-[(4-benzyl-2-morpholinyl)methyl]benzamide
反応式
[NH2:1][CH2:2][CH:3]1[O:8][CH2:7][CH2:6][N:5]([CH2:9][C:10]2[CH:15]=[CH:14][CH:13]=[CH:12][CH:11]=2)[CH2:4]1.[CH2:16]1[O:27][C:26]2[C:18](=[C:19]([CH:23]=[CH:24][CH:25]=2)[C:20](O)=[O:21])[O:17]1.NCC1OCCN(CC2C=CC(C#N)=CC=2)C1.NC1C(Cl)=CC(C(O)=O)=C(OC)C=1>>[CH2:16]1[O:27][C:26]2[C:18](=[C:19]([CH:23]=[CH:24][CH:25]=2)[C:20]([NH:1][CH2:2][CH:3]2[O:8][CH2:7][CH2:6][N:5]([CH2:9][C:10]3[CH:15]=[CH:14][CH:13]=[CH:12][CH:11]=3)[CH2:4]2)=[O:21])[O:17]1参加物
5
実験手順
The title compound is prepared in substantially the same manner as in Example 6(1), using 2-aminomethyl-4-benzylmorpholine and 2,3-methylenedioxybenzoic acid, respectively, in place of 2-aminomethyl-4-(4-cyanobenzyl)morpholine and 4-amino-5-chloro-2-methoxybenzoic acid in Example 6(1). The free base thus obtained is treated in substantially the same manner as in Example 6(2) to give the fumarate 1/4 hydrate of the title compound, mp 144°-146° C. (recrystallized from ethanol).