1-B-D-AURABINOFURANOSYL CYTOSINE DERIVATIVES AND PROCESS FOR M AKING SAME

摘要

1335493 Arabinofuranosyl-cytosines SYNTEX CORP 19 April 1971 [19 March 1970] 49147/72 Divided out of 1335492 Heading C2C The invention comprises (1) novel compounds of Formulae VII and VIII (in which each of R1' and R2' is H, alkyl or cycloalkyl and Y2 is OH, Cl or Br) and pharmaceutically acceptable salts thereof, and (2) a process for the preparation of arabinofuranosyl compounds of Formula C in which each of R1 and R2 is H, alkyl, cycloalkyl, aryl, aralkyl or alkaryl, Y1 is H, OH, halogen, etherified OH, NH 2 , alkylamino or azido, W is O or S and Z is a group of Formula IV, V or VI in which R4 is H, alkyl, cycloalkyl, hydroxyalkyl, haloalkyl, N 3 , NO 2 , NH 2 , alkylamino or acylamino, and R5 is H or CH 3 , provided that when Z is a group of Formula V or VI, Y is OH, Cl or Br, each of R1 and R2 is H, alkyl or cycloalkyl and W is O, and that when W is S, each of R1 and R2 is H, Y is OH and Z is the group of Formula IX are prepared by alkaline hydrolysis of compounds of Formula I in which R1, R2, R4, R5 and Z are as defined above for compounds C except that R4 may also be halogen, Y is the same as Y1 or is an acyloxy, or alkoxycarbonyloxy group, and R3 is alkyl, aryl, cycloalkyl, heterocyclyl, aralkyl or alkaryl. Pharmaceutical compositions having antiviral and cytotoxic activity comprise a compound of Formula I or II or a pharmaceutically acceptable salt thereof together with a carrier.