Hydrochloric Acid → N-(7-(2-Fluoro-4-iodophenylamino)-8-fluoro-4-methylquinazolin-6-yl)-1-(2-hydroxyethyl)cyclopropane-1-sulfonamide

HRID 558254Notizen

Reaktionsgleichung

Reaktionsgleichung von HRID 558254
[F:1][C:2]1[CH:7]=[C:6]([I:8])[CH:5]=[CH:4][C:3]=1[NH:9][C:10]1[C:19]([F:20])=[C:18]2[C:13]([C:14]([CH3:21])=[N:15][CH:16]=[N:17]2)=[CH:12][C:11]=1[NH:22][S:23]([C:26]1([CH2:29][CH2:30][O:31][Si](C(C)(C)C)(C)C)[CH2:28][CH2:27]1)(=[O:25])=[O:24].Cl>C1COCC1>[F:1][C:2]1[CH:7]=[C:6]([I:8])[CH:5]=[CH:4][C:3]=1[NH:9][C:10]1[C:19]([F:20])=[C:18]2[C:13]([C:14]([CH3:21])=[N:15][CH:16]=[N:17]2)=[CH:12][C:11]=1[NH:22][S:23]([C:26]1([CH2:29][CH2:30][OH:31])[CH2:28][CH2:27]1)(=[O:24])=[O:25]

Komponenten

4

Edukt 2

HCID 313Hydrochloric AcidHCID 59519447N-(7-(2-Fluoro-4-iodophenylamino)-8-fluoro-4-methylquinazolin-6-yl)-1-(2-(tert-butyldimethylsilyloxy)ethyl)cyclopropane-1-sulfonamide

Produkt 1

HCID 25161112N-(7-(2-Fluoro-4-iodophenylamino)-8-fluoro-4-methylquinazolin-6-yl)-1-(2-hydroxyethyl)cyclopropane-1-sulfonamide

Reagenzien, Katalysatoren, Lösungsmittel 1

HCID 8028TetrahydrofuranLösungsmittel

Versuchsvorschrift

To a solution of N-(7-(2-fluoro-4-iodophenylamino)-8-fluoro-4-methylquinazolin-6-yl)-1-(2-(tert-butyldimethylsilyloxy)ethyl)cyclopropane-1-sulfonamide (36 mg, 0.056 mmol) in THF (2 ml) is added HCl (0.18 ml, 1.2 N in H2O, 0.22 mmol). After stirring for 1 h, the reaction is quenched with saturated aqueous NaHCO3 solution (3 ml) and extracted with EtOAc (2×10 ml). The combined organic solution is dried over Na2SO4 and concentrated. Silica gel chromatography yields the title compound.

Aufarbeitung

  1. customthe reaction is quenched with saturated aqueous NaHCO3 solution (3 ml)
  2. extractionextracted with EtOAc (2×10 ml)
  3. dry with materialThe combined organic solution is dried over Na2SO4
  4. concentrationconcentrated

Quellen und Nachweise

ORD-Eintrag
ord-e362b0fa5b0948878718c29bc00b0073
Quelldatensatz
uspto-grants-2011_11
Patentnummer
US08063049B2

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