| 摘要 |
An improved process for preparing gemcitabine or salts thereof, comprising the following steps, dissolved 2-Deoxy-2,2- difluoro-D-ribofuranose-3,5-dibenzoate in an organic solvent and allowed to cool to 0 to 10 degree centigrade temperature, stirred for a period of 1 to 2 hours to this triethylamine is added for a period of 2 to 10 minutes, an indigenous protecting compound added under constant stirring, solvents were distilled off, and to the residual volume IN HCL is added until to form a clear solution adjusted the PH of about 2, further to this an ethyl acetate was added followed by washing the organic phase using NaHCo3, water and brine solution, the organic phase was dried over MgSo4, concentrated the above reaction mixture under reduced pressure to obtain a crude 2-deoxy-2,2-difluoro-D- riboufuranose-3,5-dibenzoate-l-arylateas an oil phase, above product is dissolved in dry methanol under constant stirring using Ion exhange resin for a period of 15 to 25 hours at 30 to 45 degree centigrade temperature, which gives pure gemcitabine hydrochloride. |
