반응 #172002

반응 방정식

(R)-3-(benzyloxy)-2-(3-bromo-4-cyanophenylamino)propanamide

5-amino-3-methylisothiazole hydrochloride

BINAP

K2CO3

→

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

용매

dioxane

반응 조건

후처리

1. 1
   기타was degassed with Ar
2. 2
   workup.ADDITIONWater and EtOAc were added
3. 3
   여과After being filtered
4. 4
   기타the organic phase was separated
5. 5
   건조dried over Na2SO4
6. 6
   농축concentrated in vacuo

실험 절차

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).

출처