4-Aminopyridine hydrochloride → 2-(4-imino-4H-pyridin-1-yl)-6-(3,5-dimethoxyphenyl)-8-ethyl-8H-pyrido[2,3-d]pyrimidin-7-one hydrochloride
Reaktionsgleichung
CS([C:4]1[N:5]=[CH:6][C:7]2[CH:13]=[C:12]([C:14]3[CH:19]=[C:18]([O:20][CH3:21])[CH:17]=[C:16]([O:22][CH3:23])[CH:15]=3)[C:11](=[O:24])[N:10]([CH2:25][CH3:26])[C:8]=2[N:9]=1)=O.[ClH:27].[NH2:28][C:29]1[CH:34]=[CH:33][N:32]=[CH:31][CH:30]=1>C(#N)C.C(O)C>[ClH:27].[NH:28]=[C:29]1[CH:34]=[CH:33][N:32]([C:4]2[N:5]=[CH:6][C:7]3[CH:13]=[C:12]([C:14]4[CH:19]=[C:18]([O:20][CH3:21])[CH:17]=[C:16]([O:22][CH3:23])[CH:15]=4)[C:11](=[O:24])[N:10]([CH2:25][CH3:26])[C:8]=3[N:9]=2)[CH:31]=[CH:30]1Komponenten
5
Edukt 2
Produkt 1
Reagenzien, Katalysatoren, Lösungsmittel 2
Reaktionsbedingungen
- Temperatur
- 40 °C
Versuchsvorschrift
To a solution of 220 g (0.59 mol) of the product of Example 2, 2-methylsulfinyl-6-(3,5-dimethoxy-phenyl)8-ethyl-8H-pyrido[2,3-d]pyrimidine-7-one, in 2 L of acetonitrile was added a solution of 100 g (0.765 mol, 1.3 eq) of 4-aminopyridine hydrochloride in 700 mL of ethanol. The mixture was heated to 40° C. and stirred for 6 hours. The mixture was then cooled to 24° C. and filtered to provide 256 g (99%) of 2-(4-imino-4H-pyridin-1-yl)-6-(3,5-dimethoxyphenyl)-8-ethyl-8H-pyrido[2,3-d]-pyrimidin-7-one hydrochloride; mp 295-300° C. (dec).
Aufarbeitung
- temperatureThe mixture was then cooled to 24° C.
- filtrationfiltered
Quellen und Nachweise
- ORD-Eintrag
- ord-95f54554223a4911bb41e59fe5bcba43
- Quelldatensatz
- uspto-grants-2005_11
- Patentnummer
- US06960662B2
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