Process for the preparation of 7 alpha-alkoxycephem derivatives

Details Process for the preparation of 7 alpha-alkoxycephem derivatives Process for the preparation of 7 alpha-alkoxycephem derivatives

1991-04-25

1993-10-19

Rizzo, Nicholas S.

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

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

540215, 540228, C07D50104

Patent

active

052546802

ABSTRACT:
There is provided a process for preparing a compound of the formula (I): ##STR1## wherein R.sub.1 is an organic residue, R.sub.2 is a hydrogen or a chlorine atom, a methoxy, ethoxy or an acetoxy group, and n represents 0, 1 or 2.
The process comprises reacting a compound of the formula (II): ##STR2## wherein R.sub.2 and n are as defined above, with an inorganic or organic nitrite, in an alcohol R.sub.1 OH, wherein R.sub.1 is as defined above, or in a mixture R.sub.1 OH-organic solvent in the presence of an inorganic or organic acid.
The compounds of the formula (I) are known intermediates in the synthesis of human leucocyte elastase inhibitors (HLE).

REFERENCES:
patent: 4093625 (1978-06-01), Commons
patent: 4456755 (1984-06-01), Sheehan
patent: 4992541 (1991-02-01), Blacklick et al.
The Journal of Organic Chemistry, vol. 54, No. 16, Aug. 4, 1989, T. J. Blacklock, et al., "A Versatile Synthesis of 1,1-Dioxo 7-Substituted Cephems: Preparation of the Human Leukocyte Elastase (HLE) Inhibitor 1,1-Dioxo-Trans-7-Methoxycephalosporanic".
James B. Doherty et al., Cephalosporin Antibiotics can be Modified to Inhibit Human Leukocyte Elastase, Nature, vol. 322, Jul. 10, 1986, 192-194, 1 p. formula.
R. J. Bonney et al., Pharmacological Profile of the Substituted Beta-lactam L-659,286: A Member of a New Class of Human PMN Elastase Inhibitors, Journal of Cellular Biochemistry 39:47-53 (1989) Cellular Proteases and Control Mechanisms 7 pages.
William K. Hagmann et al., Inhibition of Human Leukocyte Elastase by C-2 Substituted Cephalosporin Sulfones, J. Med. Chem. 24 (1989) pp. 599-603, Paris.

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