Title:
PRODUCTION OF HALOGENATED BETA-LACTAM COMPOUND
Document Type and Number:
Japanese Patent JP3236261
Kind Code:
B2
Abstract:
PROBLEM TO BE SOLVED: To efficiently obtain the subject compound useful as an intermediate for synthesizing medicines, etc., in a high yield without using an organic solvent having the problems of safety and environmental pollution by reacting a specified amino compound with nitrous acid, etc., in the presence of a halogen molecule in water under an acidic condition in a slurry dispersion state.
SOLUTION: This method for producing a halogenated β-lactam compound of formula IV (X1 is H or the like; X2 is a halogen) (for example, 6, 6- dibromopenicillanic acid) comprises reacting (A) a β-lactam-based amino compound of formula I [(n) is 0-2; A is a group of formula II or a group of formula III ; R1 and R2 are each H or the like] (for example, 6-aminopenicillanic acid) with (D) nitrous acid or a nitrite salt (for example, sodium nitrite) in the presence of (B) a halogen molecule such as bromine in water under an acidic condition using (C) an acid such as hydrobromic acid in a slurry dispersion state usually at atmospheric pressure preferably at a temperature of -5 to 6°C for 12-24 hrs. The component B, the component C and the component D are preferably used in amounts of 2-6 equivalents, 1.5-6 equivalents and 2-6 equivalents, respectively, based on the amount of the component A.
Inventors:
Akihiro Shimabayashi
Ichiro Kawahara
Shigetoshi Taniguchi
Hiroaki Asai
Ichiro Kawahara
Shigetoshi Taniguchi
Hiroaki Asai
Application Number:
JP11618798A
Publication Date:
December 10, 2001
Filing Date:
April 09, 1998
Export Citation:
Assignee:
Otsuka Chemical Co., Ltd.
International Classes:
C07D499/87; C07D499/00; C07D499/04; C07D499/10; C07D499/86; C07D499/865; C07D499/897; C07D501/00; C07D501/04; C07D501/16; C07D501/59; (IPC1-7): C07D501/04; C07D499/86; C07D499/87; C07D499/897
Domestic Patent References:
| JP5572115A |
Attorney, Agent or Firm:
Iwao Tamura