تفاعل #60256

معادلة التفاعل

4,5-Diamino-2-(2-chloro-phenylamino)-3-fluoro-benzoic acid methyl ester

formamidine acetate

→

pure desired product

المردود 85.0%

6-(2-Chloro-phenylamino)-7-fluoro-3H-benzoimidazole-5-carboxylic acid methyl ester

المردود 85.0%

المذيبات

ethyl acetate

EtOH

ظروف التفاعل

المعالجة

1. 1
   درجة الحرارةThe reaction mixture is heated to reflux
2. 2
   غسيلThe organic layer is washed with water, saturated NaHCO3, 10% K2CO3 and brine
3. 3
   تجفيفThe organic layer is dried (MgSO4)
4. 4
   تركيزconcentrated under reduced pressure

الإجراء التجريبي

4,5-Diamino-2-(2-chloro-phenylamino)-3-fluoro-benzoic acid methyl ester 6a (0.125 g, 0.404 mmol) is suspended in EtOH (2 mL) and formamidine acetate (63 mg, 0.605 mmol) is added. The reaction mixture is heated to reflux. After 16 hours, the reaction mixture is cooled to room temperature and diluted with ethyl acetate. The organic layer is washed with water, saturated NaHCO3, 10% K2CO3 and brine. The organic layer is dried (MgSO4) and concentrated under reduced pressure to give 0.109 g (85%) pure desired product.

المصدر