(R)-3-methylisothiazolidine 1,1-dioxide → (R)-[4-(2,4-dimethylphenyl)piperazin-1-yl][6-(3-methyl-1,1-dioxo-1lambda6-isothiazolidin-2-yl)pyridin-3-yl]methanone

HRID 2411533Notes

Reaction equation

HRID 2411533 reaction equation
[CH3:1][C:2]1[CH:7]=[C:6]([CH3:8])[CH:5]=[CH:4][C:3]=1[N:9]1[CH2:14][CH2:13][N:12]([C:15]([C:17]2[CH:18]=[N:19][C:20](I)=[CH:21][CH:22]=2)=[O:16])[CH2:11][CH2:10]1.[CH3:24][C@@H:25]1[CH2:29][CH2:28][S:27](=[O:31])(=[O:30])[NH:26]1>>[CH3:1][C:2]1[CH:7]=[C:6]([CH3:8])[CH:5]=[CH:4][C:3]=1[N:9]1[CH2:14][CH2:13][N:12]([C:15]([C:17]2[CH:18]=[N:19][C:20]([N:26]3[C@H:25]([CH3:24])[CH2:29][CH2:28][S:27]3(=[O:31])=[O:30])=[CH:21][CH:22]=2)=[O:16])[CH2:11][CH2:10]1

Participants

3

Reactant 2

HCID 16664802(R)-3-methylisothiazolidine 1,1-dioxideHCID 86676763[4-(2,4-Dimethylphenyl)piperazin-1-yl](6-iodopyridin-3-yl)methanone

Product 1

HCID 71253168(R)-[4-(2,4-dimethylphenyl)piperazin-1-yl][6-(3-methyl-1,1-dioxo-1lambda6-isothiazolidin-2-yl)pyridin-3-yl]methanoneYield 29.4%

Procedure

Using [4-(2,4-dimethylphenyl)piperazin-1-yl](6-iodopyridin-3-yl)methanone (341 mg) described in Preparation Example 162 and (R)-3-methylisothiazolidine 1,1-dioxide (123 mg) described in Preparation Example 2 and by the reaction and treatment in the same manner as in Example 1, the title compound (102 mg) was obtained.

Workup

  1. customdescribed in Preparation Example 2 and by the reaction and treatment in the same manner as in Example 1

Sources & evidence

ORD record
ord-2d050b6630f6470ca6f2c502a77d6cf7
Source dataset
uspto-grants-2014_08
Patent number
US08816079B2

Reaction notes

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