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HuagongsheHuagongshe Chemie-Druckbericht · Nur für Forschungszwecke
HRID 450368Erstellt: 25. Oktober 2026

Diisopropylethylamine → N4-(5-Cyclopropyl-1H-pyrazol-3-yl)-N2-[(1S)-1-(5-fluoropyridin-2-yl)ethyl]-5-nitropyrimidine-2,4-diamine

https://huagongshe.com/reaction/450368

Reaktionsgleichung

Beteiligte Stoffe

RolleNameHCIDEinwaage
EduktDiisopropylethylamineHCID 81531—
Edukt(S)-1-(5-fluoropyridin-2-yl)ethanamine hydrochlorideHCID 67123789—
Edukt2-chloro-N-(5-cyclopropyl-1H-pyrazol-3-yl)-5-nitro-pyrimidin-4-amineHCID 86621766—
Lösungsmittel1-ButanolHCID 263—
LösungsmittelEthyl AcetateHCID 8857—
ProduktN4-(5-Cyclopropyl-1H-pyrazol-3-yl)-N2-[(1S)-1-(5-fluoropyridin-2-yl)ethyl]-5-nitropyrimidine-2,4-diamineHCID 8664927862,6%

Reaktionsbedingungen

Temperatur70 °C

Reaktionsschritte

A mixture of 2-chloro-N-(5-cyclopropyl-1H-pyrazol-3-yl)-5-nitropyrimidin-4-amine (Intermediate 17, 0.35 g) and [(1S)-1-(5-fluoropyridin-2-yl)ethyl]amine hydrochloride (Intermediate 5, 0.25 g) in n-BuOH (10 mL) with diisopropylethylamine (1 mL) was stirred at 70° C. for 4 hours. The resulting mixture was diluted with ethyl acetate (20 mL), and washed with brine (10 mL×3). The organic layer was dried and concentrated. The resulting residue was separated by silica gel column (Hexane/Ethyl acetate) to yield 0.3 g of desired product. MS (electrospray): 385 (M+1) for C17H16FN8O2.

Herkunft & Nachweise

DOI10.6084/m9.figshare.5104873.v1
PatentnummerUS08486966B2
Quelldatensatzuspto-grants-2013_07
ORD IDord-a37ae4dc14f246f4ac0b10f51246200d
Quellennotizuspto-grants-2013_07