Intermediates for use in the preparation of cephalosporin antibi

Organic compounds -- part of the class 532-570 series – Organic compounds – Chalcogen in the nitrogen containing substituent

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424246, 544 25, C07D50118

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active

043693130

ABSTRACT:
(6R,7R)-7-amino-3-(1-pyridiniummethyl)ceph-3-em-4-carboxylate dihydrochloride and its solvates are prepared in substantially pure form and can be acylated by conventional methods to yield a wide variety of cephalosporin antibiotics. The dihydrochloride is advantageously prepared in the form of its crystalline dihydrate. Processes for the preparation of the dihydrochloride and its solvates are described.
The dihydrochloride and its solvates are particularly useful in the preparation of (6R,7R)-7-[(Z)-2-(2-aminothiazol-4-yl)-2-(2-carboxyprop-2-oxyimino)acetami do]-3-(1-pyridiniummethyl)ceph-3-em-4-carboxylate, in the course of the preparation of which the novel N,N-dimethylformamide solvate of (6R,7R)-7-[(Z)-2-(2-tritylaminothiazol-4-yl)-2-(2-t-butoxyprop-2-oxyimino) acetamido[-3-(1-pyridiniummethyl)ceph-3-em-4-carboxylate may be isolated in substantially pure crystalline form.

REFERENCES:
patent: 3207755 (1965-09-01), Abraham et al.
patent: 3234224 (1966-02-01), Schenicer et al.
patent: 3280118 (1966-10-01), Eardley et al.
patent: 3422099 (1969-01-01), Crast

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