Title:
NOVEL PREPARATION OF CEPHALOSPORINE DERIVATIVE
Document Type and Number:
Japanese Patent JP2625647
Kind Code:
B2
Abstract:
PURPOSE: To obtain a cephalosporine deriv. useful as antibiotics without isolating individual intermediate products through conversion of a specified aminocephalosporanic acid to an N,O-bissilylated deriv.
CONSTITUTION: 7-Aminocephalosporanic acid (7-ACA) represented by formula V or a deriv. thereof is converted to an N,0-bis-silylated deriv. thereof represented by formula IV which is then reacted with an iodization reagent (e.g. trimethyliodosilane) to give a 3-iodomethyl compd. represented by formula III. Further, a nucleophilic reaction reagent (e.g. pyridine) is added to provide a desired 3-substituted deriv. of N,O-bis-silylated-7-ACA represented by formula II. This is deprotected. Alternatively, an acylation agent capable of introducing a desired acyl group into the 7-position is allowed to act thereon, followed by deprotection. Thus, the contemplated compd. represented by formula I is obtd.
Inventors:
Gerd Aschel
Heinrich Thaler
Johannes Ludeschel
Heinrich Thaler
Johannes Ludeschel
Application Number:
JP28950694A
Publication Date:
July 02, 1997
Filing Date:
November 24, 1994
Export Citation:
Assignee:
Biohemie Gesellschaft Mitt Beschlenktel Haftung
International Classes:
C07D501/00; C07D501/02; C07D501/04; C07F7/10; C07D501/18; C07D501/24; C07D501/46; C07F7/12; C07F7/18; (IPC1-7): C07D501/04; C07D501/18; C07F7/18
Domestic Patent References:
| JP56131590A | ||||
| JP5359689A |
Foreign References:
| DE3316798A1 |
Attorney, Agent or Firm:
Aoyama Ryo (1 person outside)