Title:
N4-(SUBSUTITUTED-OXYCARBONYL)-5'-DEOXY-5-FLUOROCYTIDINE DERIVATIVE
Document Type and Number:
Japanese Patent JP2501297
Kind Code:
B2
Abstract:
PURPOSE: To provide a new N4-(substituted-oxycarbonyl)-5'-deoxy-5-fluorocytidine derivative, useful for antitumor agents as precusors of 5-fluorouracil and having less enterotoxicity.
CONSTITUTION: By dissolving 5'-deoxy-5-fluorocytidine in dried pyridine, adding an acid anhydride to the mixture at 0°C under stirring to react with each other to obtain 2',3'-di-O-acyl-5'-deoxy-5-fluorocytidine and adding dropwise of a compound of formula R1OCOCl (wherein R1 represents a 4-7C hydrocarbon or the like) (e.g. n-propylchloroformate) to the mixture under ice-cooling, the objective derivative of formula II (wherein R2 represents a hydrogen or a group easily hydrolyzable under phsiological condition) (e.g. 2',3'-di-O-acetyl-5'-deoxy-5-fluoro- N4-(proxycarbonyl)cytidine or the like) useful for antitumor agent is obtained.
Inventors:
ARASAKI MOTOHIRO
ISHIZUKA HIDEO
KURUMA ISAMU
MIWA MASANORI
MURAZAKI CHIKAKO
NIIMA NOBUO
UMEDA ISAO
ISHIZUKA HIDEO
KURUMA ISAMU
MIWA MASANORI
MURAZAKI CHIKAKO
NIIMA NOBUO
UMEDA ISAO
Application Number:
JP34281293A
Publication Date:
May 29, 1996
Filing Date:
December 16, 1993
Export Citation:
Assignee:
HOFFMANN LA ROCHE
International Classes:
A61K31/305; A61K31/7042; A61K31/70; A61K31/7052; A61K31/7064; A61K31/7068; A61P35/00; C07H19/06; C07D239/00; (IPC1-7): C07H19/06; A61K31/70
Domestic Patent References:
| JP1153696A |
Attorney, Agent or Firm:
Heiyoshi Odashima