(S)-3-benzyloxymethylisothiazolidine 1,1-dioxide → (S)-[4-(5-cyclopropyl-3-methylpyridin-2-yl)piperazin-1-yl][2-fluoro-4-(3-hydroxymethyl-1,1-dioxo-1lambda6-isothiazolidin-2-yl)phenyl]methanone

HRID 2411441Notizen

Reaktionsgleichung

Reaktionsgleichung von HRID 2411441
C([O:8][CH2:9][C@@H:10]1[CH2:14][CH2:13][S:12](=[O:16])(=[O:15])[NH:11]1)C1C=CC=CC=1.Br[C:18]1[CH:23]=[CH:22][C:21]([C:24]([N:26]2[CH2:31][CH2:30][N:29]([C:32]3[C:37]([CH3:38])=[CH:36][C:35]([CH:39]4[CH2:41][CH2:40]4)=[CH:34][N:33]=3)[CH2:28][CH2:27]2)=[O:25])=[C:20]([F:42])[CH:19]=1>>[CH:39]1([C:35]2[CH:36]=[C:37]([CH3:38])[C:32]([N:29]3[CH2:28][CH2:27][N:26]([C:24]([C:21]4[CH:22]=[CH:23][C:18]([N:11]5[C@H:10]([CH2:9][OH:8])[CH2:14][CH2:13][S:12]5(=[O:15])=[O:16])=[CH:19][C:20]=4[F:42])=[O:25])[CH2:31][CH2:30]3)=[N:33][CH:34]=2)[CH2:40][CH2:41]1

Komponenten

3

Edukt 2

HCID 16664117(S)-3-benzyloxymethylisothiazolidine 1,1-dioxideHCID 58484842(4-Bromo-2-fluorophenyl)[4-(5-cyclopropyl-3-methylpyridin-2-yl)piperazin-1-yl]methanone

Produkt 1

HCID 71253189(S)-[4-(5-cyclopropyl-3-methylpyridin-2-yl)piperazin-1-yl][2-fluoro-4-(3-hydroxymethyl-1,1-dioxo-1lambda6-isothiazolidin-2-yl)phenyl]methanoneAusbeute 10 %

Versuchsvorschrift

Using (S)-3-benzyloxymethylisothiazolidine 1,1-dioxide (241 mg) described in Preparation Example 1 and (4-bromo-2-fluorophenyl)[4-(5-cyclopropyl-3-methylpyridin-2-yl)piperazin-1-yl]methanone (418 mg) described in Preparation Example 121 and by the reaction and treatment in the same manner as in Example 32, the title compound (49 mg) was obtained.

Aufarbeitung

  1. customdescribed in Preparation Example 121 and by the reaction and treatment in the same manner as in Example 32

Quellen und Nachweise

ORD-Eintrag
ord-ed3c8502a78647d387d1bdc81c682dd9
Quelldatensatz
uspto-grants-2014_08
Patentnummer
US08816079B2

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