Lek, Tovarna Farmacevtskih in Kemicnih Izdelkov, D.d.

Lek, Tovarna Farmacevtskih in Kemicnik Izdelkov

Darja Jereb

Natasa H Milac

Natasa Hafner Milac

Boris Rusjakovski

Igor Langof

Sandi Borisek

An improved process of synthesis of 5-methoxy-2-&lsqb;(4-methoxy-3,5-dimethyl-2-pyridyl)methyl&rsqb;sulfinyl-1H-benzimidazole (omeprazole) by oxidation of 5-methoxy-2-&lsqb;&lsqb;(4-methoxy-3,5-dimethyl-2-pyridyl)methyl&rsqb;thio&rsqb;benzimidazole with 3-chloroperoxy-benzoic acid in ethyl acetate wherein omeprazole is poorly soluble, at a temperature between &minus;10&deg; C. and 5&deg; C. is disclosed. The second step is a purification of the crude product by dissolution and reprecipitation of the final product.

Process of synthesis of 5-methoxy- 2-&lsqb;(4-methoxy-3,5-dimethy-2-pyridyl)methyl&rsqb;sulfiny-1h-benzimidazole

A new and improved process for the preparation of ceftriaxon disodium salt hemiheptahydrate of formula I ##STR1## is described, wherein 7-amino-3-{[(2,5-dihydro-6-hydroxy-2-methyl-5-oxo-as-triazin-3-yl)thio]met hyl}-3-cephem-4-carboxylic acid disodium salt is converted with a reactive 2-(2-aminothiazol-4-yl)-2-syn-metoxyimino acetic acid derivative such as 2-benzo-thiazolyl-thio ester in a water solution and in the presence of a suitable inert organic solvent such as acetone, at a temperature between 0.degree. C. and 40.degree. C. and then the desired compound is isolated in a very pure form and with a high total yield. Ceftriaxon is a cephalosporin antibiotic of the third generation for parenteral application and a valuable agent for the treatment of heavy infections.

Process for the preparation of ceftriaxon disodium salt hemiheptahydrate

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Radomlje, Slovenia

Darja Jereb