Zurück
HuagongsheHuagongshe Chemie-Druckbericht · Nur für Forschungszwecke
HRID 2201051Erstellt: 23. Oktober 2026

Potassium Carbonate → (R)-3-(benzyloxy)-2-(4-cyano-3-(3-methylisothiazol-5-ylamino)phenylamino)propanamide

https://huagongshe.com/de/reaction/2201051

Reaktionsgleichung

Beteiligte Stoffe

RolleNameHCIDEinwaage
EduktPotassium CarbonateHCID 11430—
EduktBinap, (A+-)-HCID 634876—
Edukt3-Methylisothiazol-5-ylamine hydrochlorideHCID 2723918—
Edukt(R)-3-(benzyloxy)-2-(3-bromo-4-cyanophenylamino)propanamideHCID 67509048—
Katalysatorpalladium(II) acetateHCID 167845—
Lösungsmittel1,4-DioxaneHCID 31275—
Produkt(R)-3-(benzyloxy)-2-(4-cyano-3-(3-methylisothiazol-5-ylamino)phenylamino)propanamideHCID 67508575—

Reaktionsschritte

A mixture of (R)-3-(benzyloxy)-2-(3-bromo-4-cyanophenylamino)propanamide (66 mg, 0.176 mmol), 5-amino-3-methylisothiazole hydrochloride (35 mg, 0.232 mmol), BINAP (20 mg, 0.032 mmol), Pd(OAc)2 (15 mg, 0.066 mmol) and K2CO3 (100 mg, 0.724 mmol) in dioxane (2 mL) was degassed with Ar, then was stirred at 120 C for 18 h. Water and EtOAc were added. After being filtered, the organic phase was separated, dried over Na2SO4, concentrated in vacuo to give (R)-3-(benzyloxy)-2-(4-cyano-3-(3-methylisothiazol-5-ylamino)phenylamino)propanamide as a crude residue (73 mg).

Herkunft & Nachweise

DOI10.6084/m9.figshare.5104873.v1
PatentnummerUS09359375B2
Quelldatensatzuspto-grants-2016_06
ORD IDord-b6d2c73669a04b86b1fb98b77f1f984e
Quellennotizuspto-grants-2016_06