(S)-3-benzyloxymethylisothiazolidine 1,1-dioxide → (S)-[4-(3-benzyloxymethyl-1,1-dioxo-1lambda6-isothiazolidin-2-yl)-2,6-difluorophenyl][4-(3,5-dimethylpyridin-2-yl)piperazin-1-yl]methanone

HRID 2411417ノート

反応式

HRID 2411417 の反応式
[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.Br[C:18]1[CH:23]=[C:22]([F:24])[C:21]([C:25]([N:27]2[CH2:32][CH2:31][N:30]([C:33]3[C:38]([CH3:39])=[CH:37][C:36]([CH3:40])=[CH:35][N:34]=3)[CH2:29][CH2:28]2)=[O:26])=[C:20]([F:41])[CH:19]=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:18]1[CH:19]=[C:20]([F:41])[C:21]([C:25]([N:27]2[CH2:32][CH2:31][N:30]([C:33]3[C:38]([CH3:39])=[CH:37][C:36]([CH3:40])=[CH:35][N:34]=3)[CH2:29][CH2:28]2)=[O:26])=[C:22]([F:24])[CH:23]=1)[C:2]1[CH:3]=[CH:4][CH:5]=[CH:6][CH:7]=1

参加物

3

反応物 2

HCID 16664117(S)-3-benzyloxymethylisothiazolidine 1,1-dioxideHCID 58484761(4-Bromo-2,6-difluorophenyl)[4-(3,5-dimethylpyridin-2-yl)piperazin-1-yl]methanone

生成物 1

HCID 71252187(S)-[4-(3-benzyloxymethyl-1,1-dioxo-1lambda6-isothiazolidin-2-yl)-2,6-difluorophenyl][4-(3,5-dimethylpyridin-2-yl)piperazin-1-yl]methanone収率 60%

実験手順

Using (S)-3-benzyloxymethylisothiazolidine 1,1-dioxide (536 mg) described in Preparation Example 1 and (4-bromo-2,6-difluorophenyl)[4-(3,5-dimethylpyridin-2-yl)piperazin-1-yl]methanone (911 mg) described in Preparation Example 111 and by the reaction and treatment in the same manner as in Example 4, the title compound (760 mg) was obtained.

後処理

  1. customdescribed in Preparation Example 111 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-1ec1c69624f24aaa9a35ceee51a674ea
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…