PURPOSE: To obtain the subject compound useful as a remedy for AIDS or its raw material by condensing a 5-substituted pyrimidine derivative to a 2- organothio-2,3-dideoxy-pentofuranose derivative in the presence of a Lewis acid and subjecting the condensation product to oxidation, thermal decomposition and deprotection.
CONSTITUTION: The objective compound of formula VI is produced by reacting a 5-substituted pyrimidine derivative of formula I [R1 to R3 are alkyl or phenyl; X is O or N (having other atoms or atomic groups); Y is H, halogen, alkyl or alkenyl] with a 2,3-dideoxy-2-(organothio)pentofuranose derivative of formula II (R4 is OH-protecting group; R5 is alkyl or phenyl; Z is halogen, acyloxy, alkyloxy or phenyloxy), oxidizing the resultant compound of formula III to obtain a compound of formula IV, subjecting the product to thermal elimination reaction and finally removing the protecting group of the obtained compound of formula V. The compound has antiviral activity against AIDS virus, etc., as it is and is also useful as a raw material for relating compounds.
KOSEKI YUKIFUMI
EBATA TAKASHI
MATSUSHITA HAJIME
NAOI YOSHITAKA
ITO KAZUO
YUKI GOSEI YAKUHIN KOGYO KK