PROCESS FOR THE PREPARATION OF 2',3'-DIDEOXYCYTIDINE (DDC), AND INTERMEDIATES USED THEREIN

摘要

The invention relates to a process for the preparation of 2',3'-dideoxycytidine, characterised in that… a) the 4-amino group of cytidine is protected with a suitable protective group,… b) the protected cytidine is bromoacetylated to give the corresponding bromoacetate derivative,… c) the bromine atom and the acetoxy group are reductively eliminated from the bromoacetate in order to obtain the 2',3'-didehydro derivative,… d) the 2',3'-didehydro derivative is hydrogenated and… e) the protective groups are removed from the 2',3'-dideoxycytidine protected on the 4-amino and 5'-hydroxy group thus resulting in order to obtain 2',3'-dideoxycytidine;… and novel intermediates occurring in this process.