Eli Lilly and Company

Frank Brown, Jr

Leonard Larry Winneroski, Jr

Gregory Alan Stephenson

Francis O Ginah

Michael Vincent Mullen

Arlette Faye Kreager

Robert Alan Forbes

The present invention provides a process for producing cefaclor crystalline bulk material having a dissolution rate in a capsule of &gE;80% in water in 30 minutes. One process route includes reducing the water content of cefaclor dihydrates or bulk material containing cefaclor dihydrate to produce a cefaclor form having a water content &lE;2%. The cefaclor having the lower water content can then be rehydrated to a water content from 3.0 to 6.5% without adversely affecting the dissolution rate. An alternative process includes the addition of at least 0.05% of cefaclor related substances to inhibit conversion of the monohydate to the dihydate form.

Process for preparing pharmaceutical bulk material having uniform dissolution

A process for the conversion of a 4-chlorosulfonyl azetidinone (a) to a 3-hydroxy-3-cephem-sulfoxide ester (d) by subjecting an intermediate comprising a tin containing Lewis acid-type Fiedel-Crafts catalyst and 3-exomethylene cepham to ozonolysis.

Process for preparing 7-substituted-amino-3-hydroxy-3-cephem-4-protected

3-Exomethylenecepham sulfoxide esters are obtained in improved yields via cyclization of 3-methyl-2-(4-chlorosulfinyl-2-oxo-3-amino-1-azetidinyl)-3-butenoic acid esters under anhydrous conditions with a Lewis acid-type Friedel-Crafts catalyst in the presence of a nitro compound, e.g., nitromethane, nitroethane, nitropropane or nitrobenzene.

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West Lafayette, IN, United States of America

Frank Brown, Jr