Title:
2-DEOXY-3-ETHYNYL-BETA-D-RIBOFURANOSYL DERIVATIVE
Document Type and Number:
Japanese Patent JP3792005
Kind Code:
B2
Abstract:
PROBLEM TO BE SOLVED: To provide the subject new nucleic acid derivative consisting of a specific 2-deoxy-3-ethynyl-β-D-ribofuranosyl derivative, exhibiting extremely strong cytocidal activity and excellent antitumor activity and useful as an antitumor agent, etc.
SOLUTION: This derivative is a new 2-deoxy-3-ethynyl-β-D-ribofuranosyl derivative expressed by the formula I (B is a nucleic acid base which may have substituent) and its ester easily decomposable in vivo or its pharmacologically permissible salt. The derivative has excellent antitumor activity and is useful as an antitumor agent, etc. The compound can be produced by reacting a compound of the formula II (R1 and R2 are each a trialkylsilyl) with an acylating agent in a solvent in the presence of a basic catalyst, desilylating the obtained acylated product, reacting the resultant compound of the formula III (Acyl is an acyl) with a tributyltin halide in the presence of azoisobutyronitrile to eliminate the 2-OH group and deacylating the product.
Inventors:
Akira Matsuda
Tasaki Sasaki
Shutou Satoshi
Tasaki Sasaki
Shutou Satoshi
Application Number:
JP12330497A
Publication Date:
June 28, 2006
Filing Date:
April 24, 1997
Export Citation:
Assignee:
Akira Matsuda
Taiho Pharmaceutical Co., Ltd.
Taiho Pharmaceutical Co., Ltd.
International Classes:
C07H19/073; A61K31/70; A61K31/7042; A61K31/7052; A61K31/7064; A61K31/7072; A61K31/7076; A61P35/00; C07H19/173; (IPC1-7): C07H19/073; A61K31/70; C07H19/173
Domestic Patent References:
| JP8041054A |
Other References:
Steven L. Bender et al.,The Journal of Organic Chemistry,米国,The American Chemical Society,1992年,Vol.57/No.6,p.1646-1647
Pierre M. J. Jung et al.,The Journal of Organic Chemistry,米国,The American Chemical Society,1997年11月28日,Vol.62/No.24,p.8309-8314
Pierre M. J. Jung et al.,The Journal of Organic Chemistry,米国,The American Chemical Society,1997年11月28日,Vol.62/No.24,p.8309-8314
Attorney, Agent or Firm:
Iwao Tamura