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 2411630Notizen

Reaktionsgleichung

Reaktionsgleichung von HRID 2411630
[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]

Komponenten

3

Edukt 2

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

Produkt 1

HCID 712518572-(4-{4-[1-(1,1-Dioxo-1lambda6-isothiazolidin-2-yl)-1-methylethyl]benzoyl}piperazin-1-yl)-5-methylnicotinonitrileAusbeute 79,7 %

Versuchsvorschrift

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.

Aufarbeitung

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

Quellen und Nachweise

ORD-Eintrag
ord-96be8cf092f04baf9533a85385219581
Quelldatensatz
uspto-grants-2014_08
Patentnummer
US08816079B2

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