(S)-3-benzyloxymethylisothiazolidine 1,1-dioxide → (S)-[4-(3-benzyloxymethyl-1,1-dioxo-1lambda6-isothiazolidin-2-yl)phenyl][4-(3,5-dimethyl-pyridin-2-yl)piperazin-1-yl]methanone
反応式
[CH2:1]([O:8][CH2:9][C@@H:10]1[CH2:14][CH2:13][S:12](=[O:16])(=[O:15])[NH:11]1)[C:2]1[CH:7]=[CH:6][CH:5]=[CH:4][CH:3]=1.[CH3:17][C:18]1[C:19]([N:25]2[CH2:30][CH2:29][N:28]([C:31]([C:33]3[CH:38]=[CH:37][C:36](I)=[CH:35][CH:34]=3)=[O:32])[CH2:27][CH2:26]2)=[N:20][CH:21]=[C:22]([CH3:24])[CH:23]=1>>[CH2:1]([O:8][CH2:9][C@@H:10]1[CH2:14][CH2:13][S:12](=[O:16])(=[O:15])[N:11]1[C:36]1[CH:37]=[CH:38][C:33]([C:31]([N:28]2[CH2:29][CH2:30][N:25]([C:19]3[C:18]([CH3:17])=[CH:23][C:22]([CH3:24])=[CH:21][N:20]=3)[CH2:26][CH2:27]2)=[O:32])=[CH:34][CH:35]=1)[C:2]1[CH:3]=[CH:4][CH:5]=[CH:6][CH:7]=1参加物
3
実験手順
Using (S)-3-benzyloxymethylisothiazolidine 1,1-dioxide (287 mg) described in Preparation Example 1 and [4-(3,5-dimethylpyridin-2-yl)piperazin-1-yl](4-iodophenyl)methanone (500 mg) described in Preparation Example 113 and by the reaction and treatment in the same manner as in Example 1, (S)-[4-(3-benzyloxymethyl-1,1-dioxo-1λ6-isothiazolidin-2-yl)phenyl][4-(3,5-dimethyl-pyridin-2-yl)piperazin-1-yl]methanone (490 mg) was obtained. The obtained (S)-[4-(3-benzyloxymethyl-1,1-dioxo-1λ6-isothiazolidin-2-yl)phenyl][4-(3,5-dimethyl-pyridin-2-yl)piperazin-1-yl]methanone (490 mg) was dissolved in ethyl acetate, 4N hydrogen chloride/ethyl acetate was added, and the precipitate was collected by filtration to give the title compound (410 mg).