PROCESS FOR THE INDUSTRIAL PRODUCTION OF 5-ALKYL-2'-DEZOXY-BETA-URIDINES BY STEREOSELECTIVE SYNTHESIS

摘要

The invention relates to a method for the stereoselective industrial preparation of 5-alkyl-2'-deoxy- beta -uridines of the general formula (I) in which R represents a straight or branched alkyl group having 1-8 carbon atoms. It is characteristic of the process that preferably protected halosugars of the general formula (III) - in which general formula (III) X' represents hydrogen or a protective group and Hal represents halogen - are added to the solution, prepared with a minimum amount of solvent, of protected 5-alkyluracids of the general formula (II) in which general formula (II) the meaning of R is the same as above and X represents a protective group - with cooling, if appropriate at temperatures below the surrounding temperature and if appropriate under reduced pressure, and the protective groups are removed in a known manner, for example by Zemplén hydrolysis.