反应详情

24.8 g (60 mmol) of rac. phenylglycine benzyl ester tosylate and 8.2 g (30 mmol) of 4-bromomethyl-2'-cyanobiphenyl are kept at 80° with stirring for 2 hours together with 15.5 g of diisopropylethylamine (Hunig base) in 60 ml of DMF. The reaction mixture is then poured into ice-water and extracted with ethyl acetate. The ethyl acetate is separated off and stirred with 2N hydrochloric acid. The hydrochloride of the title compound which precipitates as an oil is separated off, converted into the base using sodium carbonate solution and further used in crude form (Rf 0.65 in system B7).

1. customare kept at 80°
2. extractionextracted with ethyl acetate
3. customThe ethyl acetate is separated off
4. customThe hydrochloride of the title compound which precipitates as an oil
5. customis separated off