Hydrochloric Acid → 1-[4-(9-Fluoro-3-phenylpyrimido[1,2-b]indazole-2-yl)phenyl]-cyclobutylamine

HRID 877052Notizen

Reaktionsgleichung

Reaktionsgleichung von HRID 877052
C(OC(=O)[NH:7][C:8]1([C:12]2[CH:17]=[CH:16][C:15]([C:18]3[C:31]([C:32]4[CH:37]=[CH:36][CH:35]=[CH:34][CH:33]=4)=[CH:30][N:21]4[N:22]=[C:23]5[C:28]([CH:27]=[C:26]([F:29])[CH:25]=[CH:24]5)=[C:20]4[N:19]=3)=[CH:14][CH:13]=2)[CH2:11][CH2:10][CH2:9]1)(C)(C)C.Cl>O1CCOCC1>[F:29][C:26]1[CH:25]=[CH:24][C:23]2[C:28](=[C:20]3[N:19]=[C:18]([C:15]4[CH:14]=[CH:13][C:12]([C:8]5([NH2:7])[CH2:9][CH2:10][CH2:11]5)=[CH:17][CH:16]=4)[C:31]([C:32]4[CH:33]=[CH:34][CH:35]=[CH:36][CH:37]=4)=[CH:30][N:21]3[N:22]=2)[CH:27]=1

Komponenten

4

Edukt 2

HCID 313Hydrochloric AcidHCID 86702529{1-[4-(9-Fluoro-3-phenylpyrimido[1,2-b]indazole-2-yl)phenyl]cyclobutyl}carbamic acid tert-butyl ester

Produkt 1

HCID 573777651-[4-(9-Fluoro-3-phenylpyrimido[1,2-b]indazole-2-yl)phenyl]-cyclobutylamineAusbeute 38,2 %

Reagenzien, Katalysatoren, Lösungsmittel 1

HCID 312751,4-DioxaneLösungsmittel2×

Versuchsvorschrift

In a second experiment 420 mg (0.83 mmol) {1-[4-(9-fluoro-3-phenylpyrimido[1,2-b]indazole-2-yl)phenyl]cyclobutyl}carbamic acid tert-butyl ester, after dissolution in 5 mL dioxane, were treated with 22 mL 4M hydrogen chloride in dioxane. The reaction mixture was worked up as described for the first experiment. The crude products of both experiments were purified by joint chromatography on amine silicagel (eluents: dichoromethane/methanol) yielding 129.5 mg of the desired product.

Aufarbeitung

  1. customThe crude products of both experiments were purified by joint chromatography on amine silicagel (eluents: dichoromethane/methanol)

Quellen und Nachweise

ORD-Eintrag
ord-591650d5eb1047fdb392c2f6e2e604ce
Quelldatensatz
uspto-grants-2015_03
Patentnummer
US08987286B2

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