1-(5-Cyclopropyl-3-methylpyridin-2-yl)piperazine hydrochloride → [4-(5-Cyclopropyl-3-methylpyridin-2-yl)piperazin-1-yl][4-(1,1-dioxo-1lambda6-isothiazolidin-2-yl)-2-methanesulfonylphenyl]methanone

HRID 2411538Notes

Reaction equation

HRID 2411538 reaction equation
[O:1]=[S:2]1(=[O:20])[CH2:6][CH2:5][CH2:4][N:3]1[C:7]1[CH:15]=[CH:14][C:10]([C:11]([OH:13])=O)=[C:9]([S:16]([CH3:19])(=[O:18])=[O:17])[CH:8]=1.Cl.[CH:22]1([C:25]2[CH:26]=[C:27]([CH3:37])[C:28]([N:31]3[CH2:36][CH2:35][NH:34][CH2:33][CH2:32]3)=[N:29][CH:30]=2)[CH2:24][CH2:23]1>>[CH:22]1([C:25]2[CH:26]=[C:27]([CH3:37])[C:28]([N:31]3[CH2:32][CH2:33][N:34]([C:11]([C:10]4[CH:14]=[CH:15][C:7]([N:3]5[CH2:4][CH2:5][CH2:6][S:2]5(=[O:1])=[O:20])=[CH:8][C:9]=4[S:16]([CH3:19])(=[O:18])=[O:17])=[O:13])[CH2:35][CH2:36]3)=[N:29][CH:30]=2)[CH2:24][CH2:23]1

Participants

3

Reactant 2

HCID 673810911-(5-Cyclopropyl-3-methylpyridin-2-yl)piperazine hydrochlorideHCID 712521084-(1,1-Dioxo-1lambda6-isothiazolidin-2-yl)-2-methanesulfonylbenzoic acid

Product 1

HCID 71251983[4-(5-Cyclopropyl-3-methylpyridin-2-yl)piperazin-1-yl][4-(1,1-dioxo-1lambda6-isothiazolidin-2-yl)-2-methanesulfonylphenyl]methanoneYield 81.8%

Procedure

Using 4-(1,1-dioxo-1λ6-isothiazolidin-2-yl)-2-methanesulfonylbenzoic acid (319 mg) described in Preparation Example 22 and 1-(5-cyclopropyl-3-methylpyridin-2-yl)piperazine hydrochloride (254 mg) described in Preparation Example 82 and by the reaction and treatment in the same manner as in Example 86, the title compound (424 mg) was obtained.

Workup

  1. customdescribed in Preparation Example 82 and by the reaction and treatment in the same manner as in Example 86

Sources & evidence

ORD record
ord-e93ca9dc58e244a8a2ab4de6e858e3e4
Source dataset
uspto-grants-2014_08
Patent number
US08816079B2

Reaction notes

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