4-[1-(1,1-Dioxo-1lambda6-isothiazolidin-2-yl)-1-methylethyl]benzoic acid → 2-(4-{4-[1-(1,1-Dioxo-1lambda6-isothiazolidin-2-yl)-1-methylethyl]benzoyl}piperazin-1-yl)-5-methylnicotinonitrile

HRID 2411630노트

반응식

HRID 2411630 반응식
[O:1]=[S:2]1(=[O:19])[CH2:6][CH2:5][CH2:4][N:3]1[C:7]([C:10]1[CH:18]=[CH:17][C:13]([C:14]([OH:16])=O)=[CH:12][CH:11]=1)([CH3:9])[CH3:8].[C:20]([C:22]1[C:23]([N:29]2[CH2:34][CH2:33][NH:32][CH2:31][CH2:30]2)=[N:24][CH:25]=[C:26]([CH3:28])[CH:27]=1)#[N:21]>>[O:19]=[S:2]1(=[O:1])[CH2:6][CH2:5][CH2:4][N:3]1[C:7]([C:10]1[CH:11]=[CH:12][C:13]([C:14]([N:32]2[CH2:33][CH2:34][N:29]([C:23]3[N:24]=[CH:25][C:26]([CH3:28])=[CH:27][C:22]=3[C:20]#[N:21])[CH2:30][CH2:31]2)=[O:16])=[CH:17][CH:18]=1)([CH3:8])[CH3:9]

참가 물질

3

반응물 2

HCID 712519654-[1-(1,1-Dioxo-1lambda6-isothiazolidin-2-yl)-1-methylethyl]benzoic acidHCID 712522894-(3-Cyano-5-methylpyridin-2-yl)piperazine

생성물 1

HCID 712518572-(4-{4-[1-(1,1-Dioxo-1lambda6-isothiazolidin-2-yl)-1-methylethyl]benzoyl}piperazin-1-yl)-5-methylnicotinonitrile수율 79.7%

실험 절차

Using 4-[1-(1,1-dioxo-1λ6-isothiazolidin-2-yl)-1-methylethyl]benzoic acid (100 mg) described in Preparation Example 39 and 4-(3-cyano-5-methylpyridin-2-yl)piperazine (51 mg) described in Preparation Example 107 and by the reaction and treatment in the same manner as in Example 87, the title compound (94 mg) was obtained.

후처리

  1. customdescribed in Preparation Example 107 and by the reaction and treatment in the same manner as in Example 87

출처 및 근거

ORD 기록
ord-96be8cf092f04baf9533a85385219581
출처 데이터셋
uspto-grants-2014_08
특허 번호
US08816079B2

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