3-(1,3-Oxazol-5-yl)aniline → 2,2,2-Trifluoro-N-{3-[3-(2-{[3-(1,3-oxazol-5-yl)phenyl]amino}-4-pyrimidinyl)pyrazolo[1,5-a]pyridin-2-yl]phenyl}acetamide hydrochloride

HRID 1157533Notizen

Reaktionsgleichung

[Cl:1][C:2]1[N:7]=[C:6]([C:8]2[C:9]([C:17]3[CH:18]=[C:19]([NH:23][C:24](=[O:29])[C:25]([F:28])([F:27])[F:26])[CH:20]=[CH:21][CH:22]=3)=[N:10][N:11]3[CH:16]=[CH:15][CH:14]=[CH:13][C:12]=23)[CH:5]=[CH:4][N:3]=1.[NH2:30][C:31]1[CH:32]=[C:33]([C:37]2[O:41][CH:40]=[N:39][CH:38]=2)[CH:34]=[CH:35][CH:36]=1>CC(O)C.Cl>[ClH:1].[F:26][C:25]([F:28])([F:27])[C:24]([NH:23][C:19]1[CH:20]=[CH:21][CH:22]=[C:17]([C:9]2[C:8]([C:6]3[CH:5]=[CH:4][N:3]=[C:2]([NH:30][C:31]4[CH:36]=[CH:35][CH:34]=[C:33]([C:37]5[O:41][CH:40]=[N:39][CH:38]=5)[CH:32]=4)[N:7]=3)=[C:12]3[CH:13]=[CH:14][CH:15]=[CH:16][N:11]3[N:10]=2)[CH:18]=1)=[O:29]

Komponenten

Reaktionsbedingungen

Temperatur: 120 °C

Versuchsvorschrift

To a mixture of N-{3-[3-(2-chloro-4-pyrimidinyl)pyrazolo[1,5-a]pyridin-2-yl]phenyl}-2,2,2-trifluoroacetamide (0.5 g, 1.2 mmol) in i-PrOH (4 mL) was added 5-(3-aminophenyl)oxazole (0.25 g, 1.56 mmol) and 2 drops of conc. HCl. The reaction was heated in a microwave to 120° C. for 40 min. and allowed to cool to rt. The resulting solid was filtered off, washed with i-PrOH and dried to give the title compound as a tan solid (0.68 g) in 98% yield. ES-LC/MS m/z=542 [M+H]+.

Aufarbeitung

temperatureto cool to rt
filtrationThe resulting solid was filtered off
washwashed with i-PrOH
customdried

Quellen und Nachweise

ORD-Eintrag: ord-5b708d425ea04c8ebe9c87a4f038f71c
Quelldatensatz: uspto-grants-2010_10
DOI: 10.6084/m9.figshare.5104873.v1
Patentnummer: US07807673B2

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