تفاعل #671004

معادلة التفاعل

N-(2-amino-6-chloro-4-pyrimidinyl)-N-[3-fluoro-4-(4-pyridinylsulfanyl)phenyl]amine

sodium carbonate

4-ethoxyphenylboronic acid

→

desired product

N-[2-amino-6-(4-ethoxyphenyl)-4-pyrimidinyl]-N-[3-fluoro-4-(4-pyridinylsulfanyl)phenyl]amine

المذيبات

toluene

ethanol

ظروف التفاعل

المعالجة

1. 1
   أخرىAt this time, the solvents were removed at reduced pressure
2. 2
   أخرىthe residue was purified by preparative silica gel with 3% MeOH in CH2Cl2

الإجراء التجريبي

A solution of N-(2-amino-6-chloro-4-pyrimidinyl)-N-[3-fluoro-4-(4-pyridinylsulfanyl)phenyl]amine from step 1 in toluene (2 mL) in ethanol (1 mL) was treated with aqueous sodium carbonate solution (2M, 0.5 mL). The mixture was then treated with 4-ethoxyphenylboronic acid (0.36 mmol), tetrakis(triphenylphosphine)-palladium (0.009 mmol), and allowed to stir at 120° C. under argon overnight. At this time, the solvents were removed at reduced pressure and the residue was purified by preparative silica gel with 3% MeOH in CH2Cl2 to afford the desired product as a white solid (21 mg).

المصدر