(2R)-2-(tetrahydro-2H-pyran-2-yloxy)propyl methanesulfonate → 6-[(5-{[(2R)-2-(methylamino)propyl]oxy}pyridin-2-yl)oxy]-N-(1-methyl-1H-pyrazol-3-yl)quinazoline-4-amine

HRID 81641

Reaktionsgleichung

Reaktionsgleichung von HRID 81641
[CH3:1][N:2]1[CH:6]=[CH:5][C:4]([NH:7][C:8]2[C:17]3[C:12](=[CH:13][CH:14]=[C:15]([O:18][C:19]4[N:24]=[CH:23][C:22]([OH:25])=[CH:21][CH:20]=4)[CH:16]=3)[N:11]=[CH:10][N:9]=2)=[N:3]1.CS(O[CH2:31][C@H:32](OC1CCCCO1)[CH3:33])(=O)=O.[CH3:41][NH2:42].O1CCCC1>>[CH3:41][NH:42][C@H:32]([CH3:33])[CH2:31][O:25][C:22]1[CH:21]=[CH:20][C:19]([O:18][C:15]2[CH:16]=[C:17]3[C:12](=[CH:13][CH:14]=2)[N:11]=[CH:10][N:9]=[C:8]3[NH:7][C:4]2[CH:5]=[CH:6][N:2]([CH3:1])[N:3]=2)=[N:24][CH:23]=1

Komponenten

4

Edukt 3

HCID 59627468(2R)-2-(tetrahydro-2H-pyran-2-yloxy)propyl methanesulfonateHCID 66615946Methylamine tetrahydrofuranHCID 684298776-({4-[(1-methyl-1H-pyrazol-3-yl)amino]quinazolin-6-yl}oxy)pyridin-3-ol

Produkt 1

HCID 595088366-[(5-{[(2R)-2-(methylamino)propyl]oxy}pyridin-2-yl)oxy]-N-(1-methyl-1H-pyrazol-3-yl)quinazoline-4-amine

Versuchsvorschrift

Using 6-({4-[(1-methyl-1H-pyrazol-3-yl)amino]quinazolin-6-yl}oxy)pyridin-3-ol obtained in Example 6-3), (2R)-2-(tetrahydro-2H-pyran-2-yloxy)propyl methanesulfonate and 2 M methylamine/tetrahydrofuran solution, and in the same manner as in Example 26 or according to a method similar to it or according to a combination thereof with an ordinary method, the entitled compound (6 mg) was obtained as a pale yellow amorphous solid.

Quellen und Nachweise

ORD-Eintrag
ord-c67919467e9f4da8beae6a58ff060b04
Quelldatensatz
uspto-grants-2014_09
Patentnummer
US08846700B2

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