Process for preparing 3-substituted methyl-3-cephem-4-carboxylic

Details Process for preparing 3-substituted methyl-3-cephem-4-carboxylic Process for preparing 3-substituted methyl-3-cephem-4-carboxylic

1989-05-22

1991-07-23

Rizzo, Nicholas S.

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

540215, 540221, C07D50104

Patent

active

050345214

ABSTRACT:
A novel process is disclosed for preparing a 3-substituted methyl-3-cephem-4-carboxylic acid or pharmaceutically acceptable salt thereof. The process comprises reacting a 3-acetoxymethyl-3-cephem-4-carboxylic acid or pharmaceutically acceptable salt thereof with a specific compound, such as a boric acid ester, an orthoester or an acetal, in the presence of at least one specific catalyst selected from the group consisting of Lewis acids or complexes thereof, proton acids and mixtures thereof. In the process, formation of impurities, such as a lactone, is sufficiently suppressed without protection of the carboxylic acid, so that the high purity desired product, i.e., a 3-substituted-methyl-3-cephem-4-carboxylic acid or pharmaceutically acceptable salt thereof, which is useful as an intermediate for various cephalosporin antibiotics having excellent antimicrobial activity, can be prepared in one step in high yield.

REFERENCES:
patent: 3658799 (1972-04-01), Eardley et al.
patent: 3665003 (1972-05-01), Kennedy et al.
patent: 3790567 (1974-02-01), Kennedy et al.
patent: 3846416 (1974-11-01), Kennedy et al.
patent: 3948906 (1976-04-01), Eardley et al.
patent: 4482710 (1984-11-01), Fujimoto et al.
Journal of Medicinal Chemistry, vol. 14, No. 2, pp. 113-116 (1971).

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