Biochimica Opos Spa

Astra Lakemedel Aktiebolag

Luigi Ratti

Leone Dall'Asta

Cefadroxil monohydrate is prepared by solubilizing 7-[D-(-)-.alpha.-benzyloxycarbonylamino-.alpha.-(p-hydroxyphenyl)acetamido ]-3-methyl-3-cephem-4-carboxylic acid by silylation or by salification in an organic solvent, subjecting the solubilized acid in the solvent to catalytic hydrogenation, separating the catalyst from the solution, and adding water to the solution at a pH of about 4 to precipitate cefadroxil monohydrate.

Method for the preparation of monohydrate

Cefatrizine 1,2-propylene glycolate is prepared by reacting p-hydroxyphenylglycine chloride hydrochloride with 7-amino-3-iodomethyl-3-cephem-4-carboxylic acid, and then reacting the thus obtained novel intermediate, 7-[D(-)-.alpha.-amino-.alpha.-(p-hydroxyphenyl)-acetamido]-3-iodomethyl-3- cephem-4-carboxylic acid, with the sodium salt of 1,2,3-triazol-4(5)-thiol in 1,2-propylene glycol. The addition of water to the reaction mixture causes the cefatrizine, 1,2-propylene glycolate to precipate.

Process for the prepartion of cefatrizine 1,2-propylene glycolate

The 6-[D(-)-alpha(4-ethyl-2,3-dioxopiperazin-1-ylcarbonylamino)-alphaphenylace tamido]penicillanic acid and the salts thereof are prepared by synthetizing the novel intermediates, thioesters of D(-)-alpha-(4-ethyl-2,3-dioxopiperazin-1-ylcarbonylamino)-alpha-phenylacet ic acid, with mercaptoheterocycles and by converting them into the desired compound by reaction with 6-amino-penicillanic acid.

Process for the preparation of

The novel compound .alpha.-bromodiethylcarbonate, its use in the preparation of 1-ethoxycarbonyloxyethyl esters of penicillins and cephalosporins, in particular bacampicillin, and improvements in the method for preparing such esters.

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Bergamo, Italy

Luigi Ratti