반응 #172011

반응 방정식

(R)-2-(3-bromo-4-cyanophenylamino)-2-phenylacetamide

5-amino-3-methylisothiazole hydrochloride

BINAP

K2CO3

→

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

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
   세척washed with brine
6. 6
   건조dried over Na2SO4
7. 7
   농축concentrated in vacuo

실험 절차

A mixture of (R)-2-(3-bromo-4-cyanophenylamino)-2-phenylacetamide (78 mg, 0.236 mmol), 5-amino-3-methylisothiazole hydrochloride (47 mg, 0.312 mmol), BINAP (30 mg, 0.048 mmol), Pd(OAc)2 (20 mg, 0.089 mmol) and K2CO3 (134 mg, 0.971 mmol) in dioxane (3 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, washed with brine, dried over Na2SO4, concentrated in vacuo to give (R)-2-(4-cyano-3-(3-methylisothiazol-5-ylamino)phenylamino)-2-phenylacetamide as a crude residue.

출처