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

HRID 2411552ノート

反応式

HRID 2411552 の反応式
[O:1]=[S:2]1(=[O:16])[CH2:6][CH2:5][CH2:4][N:3]1[C:7]1[CH:15]=[CH:14][C:10]([C:11]([OH:13])=O)=[CH:9][CH:8]=1.[CH:17]1([C:20]2[C:21]([N:30]3[CH2:35][CH2:34][NH:33][CH2:32][CH2:31]3)=[N:22][CH:23]=[C:24]([C:26]([F:29])([F:28])[F:27])[CH:25]=2)[CH2:19][CH2:18]1>>[CH:17]1([C:20]2[C:21]([N:30]3[CH2:35][CH2:34][N:33]([C:11]([C:10]4[CH:9]=[CH:8][C:7]([N:3]5[CH2:4][CH2:5][CH2:6][S:2]5(=[O:1])=[O:16])=[CH:15][CH:14]=4)=[O:13])[CH2:32][CH2:31]3)=[N:22][CH:23]=[C:24]([C:26]([F:29])([F:27])[F:28])[CH:25]=2)[CH2:18][CH2:19]1

参加物

3

反応物 2

HCID 66250114-(1,1-Dioxo-1,2-thiazolidin-2-yl)benzoic acidHCID 584847721-(3-Cyclopropyl-5-trifluoromethylpyridin-2-yl)piperazine

生成物 1

HCID 71253108[4-(3-Cyclopropyl-5-trifluoromethylpyridin-2-yl)piperazin-1-yl][4-(1,1-dioxo-1lambda6-isothiazolidin-2-yl)phenyl]methanone収率 81.2%

実験手順

Using 4-(1,1-dioxo-1λ6-isothiazolidin-2-yl)benzoic acid (241 mg) described in Preparation Example 16 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 (401 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-740cf95ec00d403b9ad8fc2e36fea111
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…