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 2411630ノート

反応式

HRID 2411630 の反応式
[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]

参加物

3

反応物 2

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

生成物 1

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

実験手順

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.

後処理

  1. customdescribed in Preparation Example 107 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-96be8cf092f04baf9533a85385219581
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…