Hydrochloric Acid → HCID 17973220, Verbindung

HRID 238109

Reaktionsgleichung

Br[C:2]1[CH:35]=[CH:34][C:5]([NH:6][C:7]2[C:16]3[C:11](=[CH:12][C:13]([O:19][CH2:20][CH:21]4CCN(C(OC(C)(C)C)=O)[CH2:23][CH2:22]4)=[C:14]([O:17][CH3:18])[CH:15]=3)[N:10]=[CH:9][N:8]=2)=[C:4]([F:36])[CH:3]=1.F[C:38]1[CH:44]=C(C)C=C[C:39]=1N.[ClH:46].[CH:47](O)(C)C>>[ClH:46].[CH2:20]([O:19][C:13]1[CH:12]=[C:11]2[C:16]([C:7]([NH:6][C:5]3[CH:34]=[CH:35][C:2]([CH3:47])=[CH:3][C:4]=3[F:36])=[N:8][CH:9]=[N:10]2)=[CH:15][C:14]=1[O:17][CH3:18])[C:21]1[CH:22]=[CH:23][CH:44]=[CH:38][CH:39]=1

Komponenten

Edukt 4

HCID 313Hydrochloric Acid

HCID 3776Isopropanol2×

HCID 679842-Fluoro-4-methylaniline

HCID 11049999tert-Butyl 4-(((4-((4-bromo-2-fluorophenyl)amino)-6-methoxyquinazolin-7-yl)oxy)methyl)piperidine-1-carboxylate

Produkt 1

HCID 17973220HCID 17973220, VerbindungAusbeute 91 %

Versuchsvorschrift

Using an analogous procedure to that described in Example 6, 7-benzyloxy-4-chloro-6-methoxyquinazoline hydrochloride (1.55 g, 5.15 mmol), (prepared, for example, as described in WO 97/22596, Example 1), was reacted with 2-fluoro-4-methylaniline (700 mg, 5.67 mmol) in isopropanol (90 ml) containing 6.2M hydrogen chloride in isopropanol (80 μl, 0.51 mmol) to give 7-benzyloxy-4-(2-fluoro-4-methylanilino)-6-methoxyquinazoline hydrochloride (2 g, 91%).

Quellen und Nachweise

ORD-Eintrag: ord-92dd6146bcee41eca7755054989ab599
Quelldatensatz: uspto-grants-2014_02
DOI: 10.6084/m9.figshare.5104873.v1
Patentnummer: US08642608B2

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