(S)-3-benzyloxymethylisothiazolidine 1,1-dioxide → (S)-[4-(3-benzyloxymethyl-1,1-dioxo-1lambda6-isothiazolidin-2-yl)-2,6-difluorophenyl][4-(3,5-dimethylpyridin-2-yl)piperazin-1-yl]methanone

HRID 2411417Notizen

Reaktionsgleichung

Reaktionsgleichung von HRID 2411417
[CH2:1]([O:8][CH2:9][C@@H:10]1[CH2:14][CH2:13][S:12](=[O:16])(=[O:15])[NH:11]1)[C:2]1[CH:7]=[CH:6][CH:5]=[CH:4][CH:3]=1.Br[C:18]1[CH:23]=[C:22]([F:24])[C:21]([C:25]([N:27]2[CH2:32][CH2:31][N:30]([C:33]3[C:38]([CH3:39])=[CH:37][C:36]([CH3:40])=[CH:35][N:34]=3)[CH2:29][CH2:28]2)=[O:26])=[C:20]([F:41])[CH:19]=1>>[CH2:1]([O:8][CH2:9][C@@H:10]1[CH2:14][CH2:13][S:12](=[O:16])(=[O:15])[N:11]1[C:18]1[CH:19]=[C:20]([F:41])[C:21]([C:25]([N:27]2[CH2:32][CH2:31][N:30]([C:33]3[C:38]([CH3:39])=[CH:37][C:36]([CH3:40])=[CH:35][N:34]=3)[CH2:29][CH2:28]2)=[O:26])=[C:22]([F:24])[CH:23]=1)[C:2]1[CH:3]=[CH:4][CH:5]=[CH:6][CH:7]=1

Komponenten

3

Edukt 2

HCID 16664117(S)-3-benzyloxymethylisothiazolidine 1,1-dioxideHCID 58484761(4-Bromo-2,6-difluorophenyl)[4-(3,5-dimethylpyridin-2-yl)piperazin-1-yl]methanone

Produkt 1

HCID 71252187(S)-[4-(3-benzyloxymethyl-1,1-dioxo-1lambda6-isothiazolidin-2-yl)-2,6-difluorophenyl][4-(3,5-dimethylpyridin-2-yl)piperazin-1-yl]methanoneAusbeute 60 %

Versuchsvorschrift

Using (S)-3-benzyloxymethylisothiazolidine 1,1-dioxide (536 mg) described in Preparation Example 1 and (4-bromo-2,6-difluorophenyl)[4-(3,5-dimethylpyridin-2-yl)piperazin-1-yl]methanone (911 mg) described in Preparation Example 111 and by the reaction and treatment in the same manner as in Example 4, the title compound (760 mg) was obtained.

Aufarbeitung

  1. customdescribed in Preparation Example 111 and by the reaction and treatment in the same manner as in Example 4

Quellen und Nachweise

ORD-Eintrag
ord-1ec1c69624f24aaa9a35ceee51a674ea
Quelldatensatz
uspto-grants-2014_08
Patentnummer
US08816079B2

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