反应详情

温度

100 °C

To 5.0 g (19 mmol) (S)-cyclopropanecarboxylic acid [1-(4-bromo-phenyl)-ethyl]-amide (WO 2012/01107) in 40 mL MeOH are added 125 mg (0.600 mmol) palladium-(II)-acetate, 620 mg (1.10 mmol) 1,1′-bis(diphenylphosphino)-ferrocene and 4.6 g (56 mmol) sodium acetate. The mixture is stirred at 100° C. and 5 bar CO atmosphere over night. After that time, the mixture is filtered over celite and the filtrate is concentrated by evaporation. The residue is purified by column chromatography (silica gel; gradient hexane/EtOAc 1:0→1:4) to yield the desired product.

1. wait5 bar CO atmosphere over night
2. filtrationAfter that time, the mixture is filtered over celite
3. concentrationthe filtrate is concentrated by evaporation
4. customThe residue is purified by column chromatography (silica gel; gradient hexane/EtOAc 1:0→1:4)