1,5-dimethyl-1H-pyrazole-3-carboxylic acid → 1,5-Dimethyl-1H-pyrazole-3-carboxylic acid [3-((4R,5R)-2-amino-5-fluoro-4-methyl-5,6-dihydro-4H-[1,3]oxazin-4-yl)-4-fluoro-phenyl]-amide

HRID 517064

Reaktionsgleichung

Reaktionsgleichung von HRID 517064
[NH2:1][C:2]1[CH:3]=[CH:4][C:5]([F:17])=[C:6]([C@:8]2([CH3:16])[C@@H:13]([F:14])[CH2:12][O:11][C:10]([NH2:15])=[N:9]2)[CH:7]=1.[CH3:18][N:19]1[C:23]([CH3:24])=[CH:22][C:21]([C:25](O)=[O:26])=[N:20]1>>[NH2:15][C:10]1[O:11][CH2:12][C@H:13]([F:14])[C@:8]([C:6]2[CH:7]=[C:2]([NH:1][C:25]([C:21]3[CH:22]=[C:23]([CH3:24])[N:19]([CH3:18])[N:20]=3)=[O:26])[CH:3]=[CH:4][C:5]=2[F:17])([CH3:16])[N:9]=1

Komponenten

3

Edukt 2

HCID 5877571,5-dimethyl-1H-pyrazole-3-carboxylic acidHCID 86672004(4R,5R)-4-(5-amino-2-fluoro-phenyl)-5-fluoro-4-methyl-5,6-dihydro-4H-[1,3]oxazin-2-ylamine

Produkt 1

HCID 665591841,5-Dimethyl-1H-pyrazole-3-carboxylic acid [3-((4R,5R)-2-amino-5-fluoro-4-methyl-5,6-dihydro-4H-[1,3]oxazin-4-yl)-4-fluoro-phenyl]-amide

Versuchsvorschrift

The condensation of (4R,5R)-4-(5-amino-2-fluoro-phenyl)-5-fluoro-4-methyl-5,6-dihydro-4H-[1,3]oxazin-2-ylamine (intermediate A8.2) and 1,5-dimethyl-1H-pyrazole-3-carboxylic acid (CAS 5744-59-2) following procedure I yielded the title compound as a white solid. MS (ISP): m/z=364.3 [M+H]+

Quellen und Nachweise

ORD-Eintrag
ord-c90338d6385f4681b94b7c3700ce8ddf
Quelldatensatz
uspto-grants-2015_08
Patentnummer
US09115098B2

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