Reaktionsgleichung
CC(=O)Nc1cc(N)c(F)cc1C1CC1.N#Cc1cnn2c(NC3COC3)cc(Cl)nc12>C1COCCO1.CC(C)c1cc(C(C)C)c(-c2ccccc2P(C(C)(C)C)C(C)(C)C)c(C(C)C)c1.O=C(/C=C/c1ccccc1)/C=C/c1ccccc1.O=C(/C=C/c1ccccc1)/C=C/c1ccccc1.O=C(/C=C/c1ccccc1)/C=C/c1ccccc1.O=C([O-])[O-].[Cs+].[Cs+].[Pd].[Pd]>CC(=O)Nc1cc(Nc2cc(NC3COC3)n3ncc(C#N)c3n2)c(F)cc1C1CC1Komponenten
Edukt 2
Produkt 1
Reagenzien, Katalysatoren, Lösungsmittel 4
Reaktionsbedingungen
- Temperatur
- 130 °C
Versuchsvorschrift
The mixture of N-(5-amino-2-cyclopropyl-4-fluorophenyl)acetamide (54.2 mg, 0.26 mmol), 5-chloro-7-(oxetan-3-ylamino)pyrazolo[1,5-a]pyrimidine-3-carbonitrile (50.0 mg, 0.20 mmol), cesium carbonate (196 mg, 0.60 mmol), Pd2(dba)3 (18.34 mg, 0.02 mmol) and di-tert-butyl(2',4',6'-triisopropylbiphenyl-2-yl)phosphine (17.01 mg, 0.04 mmol) sealed with microwave vial was degassed and refilled with argon 3 times. Then the degassed dioxane (4 mL) was added. The resulting solution was heated at 130°C for 30 mins in microwave. After removed all the solvents, the crude residue was purified by chromatography (100% EtOAc to 3% MeOH in EtOAc). N-(5-(3-cyano-7-(oxetan-3-ylamino)pyrazolo[1,5-a]pyrimidin-5-ylamino)-2-cyclopropyl-4-fluorophenyl)acetamide (10.00 mg, 11.85 %) was obtained.
Quellen und Nachweise
- ORD-Eintrag
- ord-f2ae1a21bc9f45a9af6696711f426a7c
- Quelldatensatz
- 750 AstraZeneca ELN dataset
- Originallink
- Quelle ansehen
Verknüpfte Notizen
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