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

HRID 2411559Notes

Reaction equation

HRID 2411559 reaction equation
[O:1]=[S:2]1(=[O:23])[CH2:6][CH2:5][CH2:4][N:3]1[C:7]1[CH:15]=[C:14]([N:16]2[CH2:20][CH2:19][CH2:18][S:17]2(=[O:22])=[O:21])[CH:13]=[CH:12][C:8]=1[C:9](O)=[O:10].Cl.[CH:25]1([C:28]2[CH:29]=[C:30]([CH3:40])[C:31]([N:34]3[CH2:39][CH2:38][NH:37][CH2:36][CH2:35]3)=[N:32][CH:33]=2)[CH2:27][CH2:26]1>>[O:23]=[S:2]1(=[O:1])[CH2:6][CH2:5][CH2:4][N:3]1[C:7]1[CH:15]=[C:14]([N:16]2[CH2:20][CH2:19][CH2:18][S:17]2(=[O:21])=[O:22])[CH:13]=[CH:12][C:8]=1[C:9]([N:37]1[CH2:36][CH2:35][N:34]([C:31]2[C:30]([CH3:40])=[CH:29][C:28]([CH:25]3[CH2:27][CH2:26]3)=[CH:33][N:32]=2)[CH2:39][CH2:38]1)=[O:10]

Participants

3

Reactant 2

HCID 673810911-(5-Cyclopropyl-3-methylpyridin-2-yl)piperazine hydrochlorideHCID 712522932,4-Bis(1,1-dioxo-1lambda6-isothiazolidin-2-yl)benzoic acid

Product 1

HCID 71252530[2,4-Bis(1,1-dioxo-1lambda6-isothiazolidin-2-yl)phenyl][4-(5-cyclopropyl-3-methylpyridin-2-yl)piperazin-1-yl]methanoneYield 37%

Procedure

Using 2,4-bis(1,1-dioxo-1λ6-isothiazolidin-2-yl)benzoic acid (200 mg) described in Preparation Example 34 and 1-(5-cyclopropyl-3-methylpyridin-2-yl)piperazine hydrochloride (141 mg) described in Preparation Example 82 and by the reaction and treatment in the same manner as in Example 86, the title compound (115 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-82f7ab3246414fe78a29e0e726e1c7a9
Source dataset
uspto-grants-2014_08
Patent number
US08816079B2

Reaction notes

Loading…