تفاعل #171999

معادلة التفاعل

(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

المذيبات

dioxane

ظروف التفاعل

المعالجة

1. 1
   أخرىwas degassed with Ar
2. 2
   workup.ADDITIONWater and EtOAc were added
3. 3
   ترشيحAfter being filtered
4. 4
   أخرىthe organic phase was separated
5. 5
   غسيلwashed with 1N HCl
6. 6
   تجفيفdried over Na2SO4
7. 7
   تركيزconcentrated in vacuo

الإجراء التجريبي

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.

المصدر