Title:
PRODUCTION OF HALOGENATED BETA-LACTAM COMPOUND
Document Type and Number:
Japanese Patent JP3775818
Kind Code:
B2
Abstract:
PURPOSE: To obtain in high yield and purity the subject compound in safe and simple operation by substituting a halogen or an eliminable group for the hydroxyl group of a halogenated β-lactam compound.
CONSTITUTION: A halogenating agent (e.g. phosphorus oxychloride) or an eliminable group-forming agent (e.g. methanesulfonyl chloride) is made to act on the hydroxyl group of a compound of formula I (R1 is H or amino; R2 is H, a halogen, lower alkoxyl, lower acyl, etc., R3 is H or a carboxyl group-protecting group; R4 is an aryl; X is a halogen; (n) is 0-2) to obtain the objective halogenated β-lactam compound of formula II (Y is a halogen or an eliminable group). The amount of the halogenating agent or eliminable groupforming agent to be used is 1-50molar times that of the compound of formula I, and the reaction is conducted in a solvent such as N,N-dimethylformamide at -80 to 80°C. The compound of formula II is useful as an intermediate for antimicrobial agents having cephalosporin skeleton with no carbon atom bound to the 3-site.
Inventors:
Torii Shigeru
Hideo Tanaka
Michio Sasaoka
Kameyama Yutaka
Hideo Tanaka
Michio Sasaoka
Kameyama Yutaka
Application Number:
JP7948595A
Publication Date:
May 17, 2006
Filing Date:
March 10, 1995
Export Citation:
Assignee:
Otsuka Chemical Holdings Co., Ltd.
International Classes:
C07D205/09; C07D205/095; C07D499/00; (IPC1-7): C07D205/09; C07D205/095
Domestic Patent References:
| JP4211055A |
Attorney, Agent or Firm:
Iwao Tamura