(4-Bromo-2-fluorophenyl) [4-(3,5,6-trimethylpyridin-2-yl)piperazin-1-yl]methanone → (S)-[2-fluoro-4-(4-methyl-1,1-dioxo-1lambda6-isothiazolidin-2-yl)phenyl][4-(3,5,6-trimethylpyridin-2-yl)piperazin-1-yl]methanone

HRID 2411442ノート

反応式

HRID 2411442 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])=[C:26]([CH3:32])[N:25]=3)[CH2:20][CH2:19]2)=[O:17])=[C:12]([F:33])[CH:11]=1>>[F:33][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])=[C:26]([CH3:32])[N:25]=2)[CH2:22][CH2:23]1)=[O:17]

参加物

3

反応物 2

HCID 58484847(4-Bromo-2-fluorophenyl) [4-(3,5,6-trimethylpyridin-2-yl)piperazin-1-yl]methanoneHCID 86676774(S)-4-methylisothiazolidine 1,1-dioxide

生成物 1

HCID 71252514(S)-[2-fluoro-4-(4-methyl-1,1-dioxo-1lambda6-isothiazolidin-2-yl)phenyl][4-(3,5,6-trimethylpyridin-2-yl)piperazin-1-yl]methanone収率 32.4%

実験手順

Using (S)-4-methylisothiazolidine 1,1-dioxide (152 mg) described in Preparation Example 4 and (4-bromo-2-fluorophenyl)[4-(3,5,6-trimethylpyridin-2-yl)piperazin-1-yl]methanone (305 mg) described in Preparation Example 128 and by the reaction and treatment in the same manner as in Example 4, the title compound (112 mg) was obtained.

後処理

  1. customdescribed in Preparation Example 128 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-af38f3ffd792415f84e1bd46790fe996
出典データセット
uspto-grants-2014_08
特許番号
US08816079B2

反応ノート

読み込み中…