Process for the preparation of cephalosporin antibiotics

Details Process for the preparation of cephalosporin antibiotics Process for the preparation of cephalosporin antibiotics

1976-05-24

1977-10-11

Rizzo, Nicholas S.

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

Organic compounds

Chalcogen in the nitrogen containing substituent

544 26, 424246, 2602391, C07D50104

Patent

active

040532860

ABSTRACT:
An improved process for preparing the compound 7.beta.-(2-thienylacetamido)-7-methoxy-3-carbamoyloxymethyl-3-cephem-4-car boxylic acid or its esters, from the compound 7.beta.-(D-5-amino-5-carboxyvaleramido)-3-carbamoyloxymethyl-7-methoxy-3-c ephem-4-carboxylic acid, by conducting the transacylation of the latter compound in the presence of commercially available alumino-silicate zeolites, also known as "molecular sieves." The process can be employed to prepare a cephalosporin with a desired 7-acylamido group from cephalosporins having a broad range of different 7-acylamido groups without having to isolate and purify a 7-amino intermediate. The final products have utility as broad spectrum antibiotics.

REFERENCES:
patent: 3775410 (1973-11-01), Christensen et al.
patent: 3780034 (1973-12-01), Christensen et al.
patent: 3859282 (1975-01-01), Cheng et al.
Karady et al., J. Am. Chem. Soc., 94 (4) 1410-1411 C(1972).

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