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 2411534노트

반응식

HRID 2411534 반응식
[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

참가 물질

3

반응물 2

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

생성물 1

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

실험 절차

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.

후처리

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

출처 및 근거

ORD 기록
ord-7ab6cfc332d34c1197d775d19b0d5df1
출처 데이터셋
uspto-grants-2014_08
특허 번호
US08816079B2

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