5-Bromo-2-chloropyrimidine → HCID 76372415, Verbindung

HRID 715858

Reaktionsgleichung

Reaktionsgleichung von HRID 715858
Cl[C:2]1[N:7]=[CH:6][C:5]([C:8]#[N:9])=[CH:4][N:3]=1.BrC1C=NC(Cl)=NC=1.[F:18][C:19]1([F:65])[CH2:24][CH2:23][CH:22]([C:25]2[C:34]3[CH:33]([O:35]CC4C=CC(OC)=CC=4)[CH2:32][C:31]([CH3:46])([CH3:45])[CH2:30][C:29]=3[N:28]=[C:27]([CH:47]3[CH2:52][CH2:51][NH:50][CH2:49][CH2:48]3)[C:26]=2[CH:53]([F:64])[C:54]2[CH:59]=[CH:58][C:57]([C:60]([F:63])([F:62])[F:61])=[CH:56][CH:55]=2)[CH2:21][CH2:20]1>>[C:8]([C:5]1[CH:4]=[N:3][C:2]([N:50]2[CH2:49][CH2:48][CH:47]([C:27]3[C:26]([CH:53]([F:64])[C:54]4[CH:59]=[CH:58][C:57]([C:60]([F:63])([F:61])[F:62])=[CH:56][CH:55]=4)=[C:25]([CH:22]4[CH2:23][CH2:24][C:19]([F:18])([F:65])[CH2:20][CH2:21]4)[C:34]4[CH:33]([OH:35])[CH2:32][C:31]([CH3:46])([CH3:45])[CH2:30][C:29]=4[N:28]=3)[CH2:52][CH2:51]2)=[N:7][CH:6]=1)#[N:9]

Komponenten

4

Edukt 3

HCID 6066655-Bromo-2-chloropyrimidineHCID 214735922-Chloro-5-pyrimidinecarbonitrileHCID 86682426(-)-4-(4,4-Difluorocyclohexyl)-3-{fluoro[4-(trifluoromethyl)phenyl]methyl}-5-[(4-methoxybenzyl)oxy]-7,7-dimethyl-2-(piperidin-4-yl)-5,6,7,8-tetrahydroquinoline

Produkt 1

HCID 76372415HCID 76372415, Verbindung

Versuchsvorschrift

Reactions similar to those of the first step of Example 2 and Example 38 were performed except for using 2-chloropyrimidine-5-carbonitrile, which was synthesized by the method described in A. Takamizawa et al., Journal of Organic Chemistry, 1964, Vol. 29, pp. 1740-1742, instead of 5-bromo-2-chloropyrimidine, and from 78 mg (0.12 mmol) of (−)-4-(4,4-Difluorocyclohexyl)-3-{fluoro[4-(trifluoromethyl)phenyl]methyl}-5-[(4-methoxybenzyl)oxy]-7,7-dimethyl-2-(piperidin-4-yl)-5,6,7,8-tetrahydroquinoline, which was prepared by a method similar to that of Reference Example 10, 60 mg of the title compound was obtained as a white solid (yield: 79%).

Aufarbeitung

  1. customwas synthesized by the method

Quellen und Nachweise

ORD-Eintrag
ord-918116f058844acf924e2901b7b36fea
Quelldatensatz
uspto-grants-2015_11
Patentnummer
US09187450B2

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