(4-Bromo-2-chlorophenyl)[4-(3,5-dimethylpyridin-2-yl)piperazin-1-yl]methanone → (S)-[2-chloro-4-(4-methyl-1,1-dioxo-1lambda6-isothiazolidin-2-yl)phenyl][4-(3,5-dimethylpyridin-2-yl)piperazin-1-yl]methanone

HRID 2411437ノート

反応式

HRID 2411437 の反応式
[CH3:1][C@@H:2]1[CH2:6][S:5](=[O:8])(=[O:7])[NH:4][CH2:3]1.Br[C:10]1[CH:15]=[CH:14][C:13]([C:16]([N:18]2[CH2:23][CH2:22][N:21]([C:24]3[C:29]([CH3:30])=[CH:28][C:27]([CH3:31])=[CH:26][N:25]=3)[CH2:20][CH2:19]2)=[O:17])=[C:12]([Cl:32])[CH:11]=1>>[Cl:32][C:12]1[CH:11]=[C:10]([N:4]2[CH2:3][C@H:2]([CH3:1])[CH2:6][S:5]2(=[O:8])=[O:7])[CH:15]=[CH:14][C:13]=1[C:16]([N:18]1[CH2:19][CH2:20][N:21]([C:24]2[C:29]([CH3:30])=[CH:28][C:27]([CH3:31])=[CH:26][N:25]=2)[CH2:22][CH2:23]1)=[O:17]

参加物

3

反応物 2

HCID 58484833(4-Bromo-2-chlorophenyl)[4-(3,5-dimethylpyridin-2-yl)piperazin-1-yl]methanoneHCID 86676774(S)-4-methylisothiazolidine 1,1-dioxide

生成物 1

HCID 71252859(S)-[2-chloro-4-(4-methyl-1,1-dioxo-1lambda6-isothiazolidin-2-yl)phenyl][4-(3,5-dimethylpyridin-2-yl)piperazin-1-yl]methanone収率 21.2%

実験手順

Using (S)-4-methylisothiazolidine 1,1-dioxide (101 mg) described in Preparation Example 4 and (4-bromo-2-chlorophenyl)[4-(3,5-dimethylpyridin-2-yl)piperazin-1-yl]methanone (204 mg) described in Preparation Example 119 and by the reaction and treatment in the same manner as in Example 4, the title compound (49 mg) was obtained.

後処理

  1. customdescribed in Preparation Example 119 and by the reaction and treatment in the same manner as in Example 4

出典と根拠

ORDレコード
ord-cb50c7631d654c16992502ef0fb31f8d
出典データセット
uspto-grants-2014_08
特許番号
US08816079B2

反応ノート

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