반응 #171999

반응 방정식

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

5-amino-3-methylisothiazole hydrochloride

BINAP

K2CO3

→

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

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 1N HCl
6. 6
   건조dried over Na2SO4
7. 7
   농축concentrated in vacuo

실험 절차

A mixture of (R)-2-(3-bromo-4-cyanophenylamino)-3-phenylpropanamide (102 mg, 0.296 mmol), 5-amino-3-methylisothiazole hydrochloride (58 mg, 0.385 mmol), BINAP (25 mg, 0.040 mmol), Pd(OAc)2 (20 mg, 0.089 mmol) and K2CO3 (150 mg, 1.08 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 1N HCl, dried over Na2SO4, concentrated in vacuo to give (R)-2-(4-cyano-3-(3-methylisothiazol-5-ylamino)phenylamino)-3-phenylpropanamide as a crude residue.

출처