تفاعل #172011

معادلة التفاعل

(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

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 brine
6. 6
   تجفيفdried over Na2SO4
7. 7
   تركيزconcentrated in vacuo

الإجراء التجريبي

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.

المصدر