Zurück
HuagongsheHuagongshe Chemie-Druckbericht · Nur für Forschungszwecke
HRID 421393Erstellt: 26. Oktober 2026

Dicyclohexylcarbodiimide → (2R)-4-{(2R)-4-[2-(2-Aminopyrimidin-5-yl)-9-isobutyl-6-morpholin-4-yl-9H-purin-8-yl]-2-methylpiperazin-1-yl}-4-oxobutan-2-ol

https://huagongshe.com/reaction/421393

Reaktionsgleichung

Beteiligte Stoffe

RolleNameHCIDEinwaage
EduktDicyclohexylcarbodiimideHCID 10868—
Edukt1-HydroxybenzotriazoleHCID 75771—
Edukt3-Hydroxybutanoic acid, (R)-HCID 92135—
Edukt5-{9-Isobutyl-8-[(3R)-3-methylpiperazin-1-yl]-6-morpholin-4-yl-9H-purin-2-yl}pyrimidin-2-amineHCID 59333543—
LösungsmittelDimethylformamideHCID 6228—
Produkt(2R)-4-{(2R)-4-[2-(2-Aminopyrimidin-5-yl)-9-isobutyl-6-morpholin-4-yl-9H-purin-8-yl]-2-methylpiperazin-1-yl}-4-oxobutan-2-olHCID 5933361950,6%

Reaktionsbedingungen

Temperatur40 °C

Reaktionsschritte

5-{9-Isobutyl-8-[(3R)-3-methylpiperazin-1-yl]-6-morpholin-4-yl-9H-purin-2-yl}pyrimidin-2-amine (150 mg, 0.33 mmol), dicyclohexylcarbodiimide (103 mg, 0.5 mmol), 1-hydroxybenzotriazole (45 mg, 0.33 mmol), and (R)-3-hydroxybutyric acid (70 mg, 0.67 mmol) were dissolved in dimethylformamide (5 ml) and the resulting mixture was stirred at 40° C. for 16 hours. The solvent was evaporated under reduced pressure and then the residue was purified by preparative HPLC (column, NOMURA Develosil Combi-RP-5; mobile phase, acetonitrile/water/formic acid) to give the title compound (90 mg, 50%) as a white solid.

Herkunft & Nachweise

DOI10.6084/m9.figshare.5104873.v1
PatentnummerUS08097622B2
Quelldatensatzuspto-grants-2012_01
ORD IDord-8c2d1d629a054d578fcc5e941b5ce966
Quellennotizuspto-grants-2012_01