Morpholine → 4-(4-(2-Carbamoylpyridin-4-yloxy)-3-fluorophenylamino)-N-(2,4-difluorophenyl)-2-morpholinopyrimidine-5-carboxamide

HRID 1986110Notizen

Reaktionsgleichung

Reaktionsgleichung von HRID 1986110
[C:1]([C:4]1[CH:9]=[C:8]([O:10][C:11]2[CH:16]=[CH:15][C:14]([NH:17][C:18]3[C:23]([C:24]([NH:26][C:27]4[CH:32]=[CH:31][C:30]([F:33])=[CH:29][C:28]=4[F:34])=[O:25])=[CH:22][N:21]=[C:20](S(C)(=O)=O)[N:19]=3)=[CH:13][C:12]=2[F:39])[CH:7]=[CH:6][N:5]=1)(=[O:3])[NH2:2].[NH:40]1[CH2:45][CH2:44][O:43][CH2:42][CH2:41]1>C1COCC1>[C:1]([C:4]1[CH:9]=[C:8]([O:10][C:11]2[CH:16]=[CH:15][C:14]([NH:17][C:18]3[C:23]([C:24]([NH:26][C:27]4[CH:32]=[CH:31][C:30]([F:33])=[CH:29][C:28]=4[F:34])=[O:25])=[CH:22][N:21]=[C:20]([N:40]4[CH2:45][CH2:44][O:43][CH2:42][CH2:41]4)[N:19]=3)=[CH:13][C:12]=2[F:39])[CH:7]=[CH:6][N:5]=1)(=[O:3])[NH2:2]

Komponenten

4

Edukt 2

HCID 8083MorpholineHCID 577213594-(4-(2-carbamoylpyridin-4-yloxy)-3-fluorophenylamino)-N-(2,4-difluorophenyl)-2-(methylsulfonyl)pyrimidine-5-carboxamide

Produkt 1

HCID 577213694-(4-(2-Carbamoylpyridin-4-yloxy)-3-fluorophenylamino)-N-(2,4-difluorophenyl)-2-morpholinopyrimidine-5-carboxamideAusbeute 75 %

Reagenzien, Katalysatoren, Lösungsmittel 1

HCID 8028TetrahydrofuranLösungsmittel

Versuchsvorschrift

To a suspension of 4-(4-(2-carbamoylpyridin-4-yloxy)-3-fluorophenylamino)-N-(2,4-difluorophenyl)-2-(methylsulfonyl)pyrimidine-5-carboxamide (75 mg, 0.13 mmol) in THF (4 mL) was added morpholine (100 mg, 1.1 mmol) and the reaction mixture was stirred 15 min. The solvent was removed in vacuo and the resulting solid was triturated in methanol/ether to give the desired product (55 mg, 75%) as a white solid. MS(ESI+) m/z 566 (M+H)+.

Aufarbeitung

  1. customThe solvent was removed in vacuo
  2. customthe resulting solid was triturated in methanol/ether

Quellen und Nachweise

ORD-Eintrag
ord-a5424d99b370422fbed424b930b68084
Quelldatensatz
uspto-grants-2009_06
Patentnummer
US07547782B2

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