Title:
2',3'-DIDEOXY-2',3'-DISUBSTITUTED NUCLEOTIDES AND THEIR PRODUCTION
Document Type and Number:
Japanese Patent JP2547125
Kind Code:
B2
Abstract:
PURPOSE: To produce the subject new compound useful, e.g. as an intermediate for production of a medicine having an antiviral activity, an antitunor activity, an antimicrobial activity, etc., by conducting a coupling reaction between a 1-thioglycoside derivative and a nucleic acid base in the presence of an activator.
CONSTITUTION: A 2',3'-dideoxy-2',3'-disubstituted nucleotide represented by formula U (R1 is an alkyl, an aryl or a halogen; R2 is an alkyl, an azide, cyano amino or a halogen; B is pyrimidine or a purine base). This compound can be efficiently synthesized through short steps by conducting a coupling reaction between a 1-lithoglycoside derivative represented by formula II (P1 is a protective group; R3 is an alkyl or an aryl) and a nucleic acid base such as a pyrimidine or a purine [example; bis(trimethylsilyl)thymine, etc.] in the presence of an activator (example; N-bromosuccinimide, etc.) and subsequently removing the protective group.
Inventors:
SUGIMURA HIDEYUKI
OOSUMI KENJI
OOSUMI KENJI
Application Number:
JP7053591A
Publication Date:
October 23, 1996
Filing Date:
March 11, 1991
Export Citation:
Assignee:
NOGUCHI KENKYUSHO
International Classes:
A61K31/52; A61K31/505; A61K31/70; A61K31/7042; A61K31/7052; A61K31/7064; A61K31/7072; A61K31/7076; A61P31/12; A61P35/00; C07D405/04; C07D473/34; C07H19/06; C07H19/16; (IPC1-7): C07D405/04; A61K31/505; A61K31/70; C07H19/06; C07H19/16