1-(4-Methyl-2-trifluoromethylphenyl)piperazine → [6-(1,1-Dioxo-1lambda6-isothiazolidin-2-yl)pyridin-3-yl][4-(4-methyl-2-trifluoromethylphenyl)piperazin-1-yl]methanone

HRID 2411534ノート

反応式

HRID 2411534 の反応式
[O:1]=[S:2]1(=[O:18])[CH2:6][CH2:5][CH2:4][N:3]1[C:7]1[CH:17]=[CH:16][C:10]([C:11]([O:13]CC)=O)=[CH:9][N:8]=1.[CH3:19][C:20]1[CH:25]=[CH:24][C:23]([N:26]2[CH2:31][CH2:30][NH:29][CH2:28][CH2:27]2)=[C:22]([C:32]([F:35])([F:34])[F:33])[CH:21]=1>>[O:18]=[S:2]1(=[O:1])[CH2:6][CH2:5][CH2:4][N:3]1[C:7]1[N:8]=[CH:9][C:10]([C:11]([N:29]2[CH2:28][CH2:27][N:26]([C:23]3[CH:24]=[CH:25][C:20]([CH3:19])=[CH:21][C:22]=3[C:32]([F:34])([F:35])[F:33])[CH2:31][CH2:30]2)=[O:13])=[CH:16][CH:17]=1

参加物

3

反応物 2

HCID 213638351-(4-Methyl-2-trifluoromethylphenyl)piperazineHCID 71251937Ethyl 6-(1,1-dioxo-1lambda6-isothiazolidin-2-yl)nicotinate

生成物 1

HCID 71252424[6-(1,1-Dioxo-1lambda6-isothiazolidin-2-yl)pyridin-3-yl][4-(4-methyl-2-trifluoromethylphenyl)piperazin-1-yl]methanone収率 27.4%

実験手順

Using ethyl 6-(1,1-dioxo-1λ6-isothiazolidin-2-yl)nicotinate (363 mg) described in Preparation Example 25 and 1-(4-methyl-2-trifluoromethylphenyl)piperazine (327 mg) described in Preparation Example 96 and by the reaction and treatment in the same manner as in Example 109, the title compound (172 mg) was obtained.

後処理

  1. customdescribed in Preparation Example 96 and by the reaction and treatment in the same manner as in Example 109

出典と根拠

ORDレコード
ord-7ab6cfc332d34c1197d775d19b0d5df1
出典データセット
uspto-grants-2014_08
特許番号
US08816079B2

反応ノート

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