Title:
ANTIVIRAL SUBSTITUTED 1,3-OXATHIOLANE
Document Type and Number:
Japanese Patent JP2000143662
Kind Code:
A
Abstract:
To provide a new substituted 1,3-oxathiolane compound capable of being easily synthesized, having low toxicity, and useful as an effective anti- human immunodeficiency virus(anti-HIV) compound.
A single enantiomer or the enantiomer mixture of a cis-2- hydroxymethyl-5-(thymin-N-1'-yl)-1,3-oxathiolane compound of formula I [R1 is H; Z is S, S=O or SO2; R2 is a group of formula II (R3 is H or a 1-6C alkyl) or the like], for example, 2-benzoyloxymethyl-5-(N4'-acetyl-cytosin-1'-yl)-1,3- oxothiolane. The compound of formula I, for example, can be obtained by reacting a 1,3-oxathiolane of formula III (L is preferably an alkoxyl, carbonyl or a halogen or the like), which is obtained from a relevant aldehyde and mercaptoacetal, with a relevant purine base or pyrimidine base using a Lewis acid or trimethylsilyl triflate in a compatible solvent, such as methyl chloride.
Inventors:
BELLEAU BERNARD
NGUYEN-BA NGHE
Application Number:
JP37006399A
Publication Date:
May 26, 2000
Filing Date:
February 08, 1990
Assignee:
IAF BIOCHEM INT
International Classes:
A61K31/39; A61K31/41; A61K31/42; A61K31/445; A61K31/495; A61K31/505; A61K31/506; A61K31/513; A61K31/519; A61K31/52; A61K31/522; A61K31/53; A61K31/54; A61P31/12; A61P31/18; C07D411/04; C07B53/00; C07D239/10; C07D239/36; C07D239/47; C07D239/54; C07D263/06; C07D327/04; C07D405/04; C07D411/02; C07D411/14; C07D473/00; C07D473/04; C07D473/16; C07D473/18; C07D473/28; C07D473/30; C07D473/32; C07D473/34; C07D473/40; C07D487/04; A61K; C07D; C07H; (IPC1-7): C07D411/04; A61K31/519; A61K31/52; A61K31/522; C07D473/16; C07D473/18; C07D473/32; C07D473/34; C07D473/40; C07D487/04
Attorney, Agent or Firm:
Aoyama Ryo (1 person outside)
