(S)-3-benzyloxymethylisothiazolidine 1,1-dioxide → (S)-[4-(5-cyclopropyl-3-methylpyridin-2-yl)piperazin-1-yl][2-fluoro-4-(3-hydroxymethyl-1,1-dioxo-1lambda6-isothiazolidin-2-yl)phenyl]methanone

HRID 2411441ノート

反応式

HRID 2411441 の反応式
C([O:8][CH2:9][C@@H:10]1[CH2:14][CH2:13][S:12](=[O:16])(=[O:15])[NH:11]1)C1C=CC=CC=1.Br[C:18]1[CH:23]=[CH:22][C:21]([C:24]([N:26]2[CH2:31][CH2:30][N:29]([C:32]3[C:37]([CH3:38])=[CH:36][C:35]([CH:39]4[CH2:41][CH2:40]4)=[CH:34][N:33]=3)[CH2:28][CH2:27]2)=[O:25])=[C:20]([F:42])[CH:19]=1>>[CH:39]1([C:35]2[CH:36]=[C:37]([CH3:38])[C:32]([N:29]3[CH2:28][CH2:27][N:26]([C:24]([C:21]4[CH:22]=[CH:23][C:18]([N:11]5[C@H:10]([CH2:9][OH:8])[CH2:14][CH2:13][S:12]5(=[O:15])=[O:16])=[CH:19][C:20]=4[F:42])=[O:25])[CH2:31][CH2:30]3)=[N:33][CH:34]=2)[CH2:40][CH2:41]1

参加物

3

反応物 2

HCID 16664117(S)-3-benzyloxymethylisothiazolidine 1,1-dioxideHCID 58484842(4-Bromo-2-fluorophenyl)[4-(5-cyclopropyl-3-methylpyridin-2-yl)piperazin-1-yl]methanone

生成物 1

HCID 71253189(S)-[4-(5-cyclopropyl-3-methylpyridin-2-yl)piperazin-1-yl][2-fluoro-4-(3-hydroxymethyl-1,1-dioxo-1lambda6-isothiazolidin-2-yl)phenyl]methanone収率 10%

実験手順

Using (S)-3-benzyloxymethylisothiazolidine 1,1-dioxide (241 mg) described in Preparation Example 1 and (4-bromo-2-fluorophenyl)[4-(5-cyclopropyl-3-methylpyridin-2-yl)piperazin-1-yl]methanone (418 mg) described in Preparation Example 121 and by the reaction and treatment in the same manner as in Example 32, the title compound (49 mg) was obtained.

後処理

  1. customdescribed in Preparation Example 121 and by the reaction and treatment in the same manner as in Example 32

出典と根拠

ORDレコード
ord-ed3c8502a78647d387d1bdc81c682dd9
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…