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 2411552노트

반응식

HRID 2411552 반응식
[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

참가 물질

3

반응물 2

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

생성물 1

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

실험 절차

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.

후처리

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

출처 및 근거

ORD 기록
ord-740cf95ec00d403b9ad8fc2e36fea111
출처 데이터셋
uspto-grants-2014_08
특허 번호
US08816079B2

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