Hydrochloric Acid → N-{3-[2-(2-Aminopyridin-4-yl)ethyl]phenyl}-2-chloro-5-fluoropyrimidin-4-amine Dihydrochloride

HRID 541856Notizen

Reaktionsgleichung

Reaktionsgleichung von HRID 541856
[Cl:1][C:2]1[N:7]=[C:6]([NH:8][C:9]2[CH:10]=[C:11]([CH2:15][CH2:16][C:17]3[CH:22]=[CH:21][N:20]=[C:19]([NH:23]C(=O)OC(C)(C)C)[CH:18]=3)[CH:12]=[CH:13][CH:14]=2)[C:5]([F:31])=[CH:4][N:3]=1.[ClH:32]>O1CCOCC1>[ClH:1].[ClH:32].[NH2:23][C:19]1[CH:18]=[C:17]([CH2:16][CH2:15][C:11]2[CH:10]=[C:9]([NH:8][C:6]3[C:5]([F:31])=[CH:4][N:3]=[C:2]([Cl:1])[N:7]=3)[CH:14]=[CH:13][CH:12]=2)[CH:22]=[CH:21][N:20]=1

Komponenten

4

Edukt 2

HCID 313Hydrochloric AcidHCID 57961852tert-Butyl [4-(2-{3-[(2-chloro-5-fluoropyrimidin-4-yl)amino]phenyl}ethyl)pyridin-2-yl]carbamate

Produkt 1

HCID 86636273N-{3-[2-(2-Aminopyridin-4-yl)ethyl]phenyl}-2-chloro-5-fluoropyrimidin-4-amine Dihydrochloride

Reagenzien, Katalysatoren, Lösungsmittel 1

HCID 312751,4-DioxaneLösungsmittel2×

Reaktionsbedingungen

Temperatur
40 °C

Versuchsvorschrift

To a mixture of tert-butyl [4-(2-{3-[(2-chloro-5-fluoropyrimidin-4-yl)amino]phenyl}ethyl)pyridin-2-yl]carbamate (88 mg, 0.20 mmol) in 1,4-dioxane (0.50 mL) was added 4 M hydrogen chloride in 1,4-dioxane (2.0 mL). The resultant reaction mixture was stirred at 40° C. for 1 hour. The reaction mixture was concentrated under vacuum to give the desired product as a very hygroscopic white powder (83 mg, 100%). LCMS for C17H16ClFN5 (M+H)+: m/z=344.1.

Aufarbeitung

  1. customThe resultant reaction mixture
  2. concentrationThe reaction mixture was concentrated under vacuum

Quellen und Nachweise

ORD-Eintrag
ord-7738fd2088b54f42abaaa30df76b2a4e
Quelldatensatz
uspto-grants-2014_10
Patentnummer
US08871753B2

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