DERIVATIVES OF NUCLEOSIDE-5'-O-HYPOPHOSPHATES AND THEIR MONO- AND DITHIOHYPOPHOSPHATE ANALOGUES AND THE PROCESS FOR THE MANUFACTURE THEREOF

摘要

The subject of the invention includes derivatives of nucleoside-5'-O-hypophosphates and their mono- and dithiohypophosphate analogues, in particular 5'-O-[ß,ß-dialkyl-(a- thiohypophosphate)]-, 5'-O -[ß,ß-dialkyl-(a,a-dithiohypophosphate)]-, 5'-O-[ß,ß-dialkyl-(a,ß- dithiohypophosphate)-, 5'-O-[ß-alkyl-(a-thiohypophosphate)]-, 5'-O-[ß-alkyl-(a,oc- dithiohypophosphate)]-, 5'-O-(a-thiohypophosphate)]- and 5'-O-(a,a- dithiohypophosphate)nucleosides of general formula 1, wherein A1 is a fluorine atom, azide or hydroxyl group, A2 is a hydrogen atom, B1 is adenine, 2-chloroadenine, 2-bromoadenine, 2-fluoroadenine, 2-iodoadenine, hypoxantine, guanine, cytosine, 5-fluorocytosine, 5- bromocytosine, 5-iodocytosine, 5-chlorocytosine, azacytosine, thymine, 5-fluorouracil, 5- bromouracil, 5-iodouracil, 5-chlorouracil, 5-(2-bromovinyl)uracil, 2-pyrimidione residue, W1 is an oxygen or carbon atom or a methylidene group, W2 is a carbon atom or A1, A2, W2 jointly represent a sulfur atom or an oxygen atom, Z1 is a hydrogen or fluorine atom or a hydroxyl group or an alkoxyl group, Z2 is a hydrogen or fluorine atom or a hydroxyl or methyl group or Z1 and Z2 jointly represent a fluoromethylene group or A1, A2, Z1 and Z2 jointly represent a carbon-carbon double bond, X1, X2 and Y represent an oxygen atom or a sulfur atom, R1 and R2 represent a simple alkyl, aryl or a hydrogen atom and the process for the manufacture thereof.