Hydrochloric Acid → (R)-N-(3-chloropropyl)-5-(2-(5-fluoro-2-oxo-1,2-dihydropyridin-3-yl)pyrrolidin-1-yl)-N-methylpyrazolo[1,5-a]pyrimidine-3-carboxamide

HRID 1426933Notizen

Reaktionsgleichung

Reaktionsgleichung von HRID 1426933
Cl.[Cl:2][CH2:3][CH2:4][CH2:5][N:6]([CH3:32])[C:7]([C:9]1[CH:10]=[N:11][N:12]2[CH:17]=[CH:16][C:15]([N:18]3[CH2:22][CH2:21][CH2:20][C@@H:19]3[C:23]3[C:24]([O:30]C)=[N:25][CH:26]=[C:27]([F:29])[CH:28]=3)=[N:14][C:13]=12)=[O:8]>C(#N)C>[Cl:2][CH2:3][CH2:4][CH2:5][N:6]([CH3:32])[C:7]([C:9]1[CH:10]=[N:11][N:12]2[CH:17]=[CH:16][C:15]([N:18]3[CH2:22][CH2:21][CH2:20][C@@H:19]3[C:23]3[C:24](=[O:30])[NH:25][CH:26]=[C:27]([F:29])[CH:28]=3)=[N:14][C:13]=12)=[O:8]

Komponenten

4

Edukt 2

HCID 313Hydrochloric AcidHCID 67470673(R)-N-(3-chloropropyl)-5-(2-(5-fluoro-2-methoxypyridin-3-yl)pyrrolidin-1-yl)-N-methylpyrazolo[1,5-a]pyrimidine-3-carboxamide

Produkt 1

HCID 67470639(R)-N-(3-chloropropyl)-5-(2-(5-fluoro-2-oxo-1,2-dihydropyridin-3-yl)pyrrolidin-1-yl)-N-methylpyrazolo[1,5-a]pyrimidine-3-carboxamideAusbeute 150 %

Reagenzien, Katalysatoren, Lösungsmittel 1

HCID 6342AcetonitrileLösungsmittel

Reaktionsbedingungen

Temperatur
90 °C

Versuchsvorschrift

A mixture of HCl (4 N dioxane, 4 mL, 16.0 mmol) and (R)-N-(3-chloropropyl)-5-(2-(5-fluoro-2-methoxypyridin-3-yl)pyrrolidin-1-yl)-N-methylpyrazolo[1,5-a]pyrimidine-3-carboxamide (100 mg, 0.224 mmol) was sealed in a pressure tube and heated at 90° C. for 90 minutes. The reaction mixture was then diluted with acetonitrile and concentrated to yield the crude product, which was carried to the next step without further purification (145 mg, 150% yield). MS (apci) m/z=433.0 (M+H).

Aufarbeitung

  1. customwas sealed in a pressure tube
  2. concentrationconcentrated

Quellen und Nachweise

ORD-Eintrag
ord-31017785c4ea47febdb8ff02f667690d
Quelldatensatz
uspto-grants-2015_01
Patentnummer
US08933084B2

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