تفاعل #85075

معادلة التفاعل

2-[4-(5-chloro-2-cyanophenyl)-5-methoxy-2-oxopyridin-1(2H)-yl]-4,4-difluorobutanoic acid

ethyl 4-aminobenzoate

DIC

→

Ethyl 4-({2-[4-(5-chloro-2-cyanophenyl)-5-methoxy-2-oxopyridin-1(2H)-yl]-4,4-difluorobutanoyl}amino)benzoate

المذيبات

dimethylformamide

ظروف التفاعل

المعالجة

1. 1
   أخرىThe crude product was purified by preparative HPLC [column
2. 2
   أخرىa further 3 min 90% acetonitrile

الإجراء التجريبي

97.0 mg (253 μmol) of 2-[4-(5-chloro-2-cyanophenyl)-5-methoxy-2-oxopyridin-1(2H)-yl]-4,4-difluorobutanoic acid (racemate), 42.0 mg (253 μmol) of ethyl 4-aminobenzoate, 36.0 mg (253 μmol) of Oxima and 39.0 μl (253 μmol) of DIC in 2.5 ml of dimethylformamide were reacted according to General Method 5B. The crude product was purified by preparative HPLC [column: Chromatorex C18, 10 μm, 125×30 mm, mobile phase: acetonitrile/0.05% formic acid gradient (0 to 3 min 10% acetonitrile, to 35 min 90% acetonitrile and a further 3 min 90% acetonitrile)]. Yield: 81.7 mg (60% of theory)

المصدر