4-(1,1-Dioxo-1,2-thiazolidin-2-yl)-2-methylbenzoic acid → [4-(3-Cyclopropyl-5-trifluoromethylpyridin-2-yl)piperazin-1-yl][4-(1,1-dioxo-1lambda6-isothiazolidin-2-yl)-2-methylphenyl]methanone

HRID 2411566ノート

反応式

HRID 2411566 の反応式
[O:1]=[S:2]1(=[O:17])[CH2:6][CH2:5][CH2:4][N:3]1[C:7]1[CH:15]=[CH:14][C:10]([C:11]([OH:13])=O)=[C:9]([CH3:16])[CH:8]=1.[CH:18]1([C:21]2[C:22]([N:31]3[CH2:36][CH2:35][NH:34][CH2:33][CH2:32]3)=[N:23][CH:24]=[C:25]([C:27]([F:30])([F:29])[F:28])[CH:26]=2)[CH2:20][CH2:19]1>>[CH:18]1([C:21]2[C:22]([N:31]3[CH2:36][CH2:35][N:34]([C:11]([C:10]4[CH:14]=[CH:15][C:7]([N:3]5[CH2:4][CH2:5][CH2:6][S:2]5(=[O:1])=[O:17])=[CH:8][C:9]=4[CH3:16])=[O:13])[CH2:33][CH2:32]3)=[N:23][CH:24]=[C:25]([C:27]([F:30])([F:28])[F:29])[CH:26]=2)[CH2:19][CH2:20]1

参加物

3

反応物 2

HCID 545952974-(1,1-Dioxo-1,2-thiazolidin-2-yl)-2-methylbenzoic acidHCID 584847721-(3-Cyclopropyl-5-trifluoromethylpyridin-2-yl)piperazine

生成物 1

HCID 71251977[4-(3-Cyclopropyl-5-trifluoromethylpyridin-2-yl)piperazin-1-yl][4-(1,1-dioxo-1lambda6-isothiazolidin-2-yl)-2-methylphenyl]methanone収率 76.8%

実験手順

Using 4-(1,1-dioxo-1λ6-isothiazolidin-2-yl)-2-methylbenzoic acid (255 mg) described in Preparation Example 29 and 1-(3-cyclopropyl-5-trifluoromethylpyridin-2-yl)piperazine (271 mg) described in Preparation Example 90 and by the reaction and treatment in the same manner as in Example 87, the title compound (390 mg) was obtained.

後処理

  1. customdescribed in Preparation Example 90 and by the reaction and treatment in the same manner as in Example 87

出典と根拠

ORDレコード
ord-40598b43f25747f59bd7d2614c078531
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…