PURPOSE: To obtain a new compd. which is useful as a therapeutic drug for AIDS and suitable for oral dose because the compd. is stable in an acid environment such as a stomach and suppresses infection by human immunodeficiency virus.
CONSTITUTION: This compd. is expressed by formula I (A is OH or NH2; B is H, CH3, CF3, CH=CHBr or a halogen), for example, 5-chloro-1-(2,3-dideoxy-2- fluoro-[β-D-threo-pentofuranosyl)cytosine. The compd. is obtd., for example, by producing a fluorodideoxy sugar expressed by formula III from a compd. expressed by formula II through a methylxanthate intermediate, then producing a 1-α-bromo deriv. from the obtd. sugar by in-situ synthesis, reacting the obtd. deriv. with a silylated pyrimidine to obtain a protected nucleoside expressed by formula IV, and then treating the compd. with a methanolic ammonia to deblock.
TSUEN KURISUTOFUAA KUU HOO
MARUKIIZU BUIKUTAA II
| JPS63303992A | 1988-12-12 |