Istituto Chemioterapico Italiano

Andrea Bottazzi

Aldo Garzia

Giorgio Vittadini

Costantino Coccoli

Domenico Pelagalli

William Ferrari

There is disclosed the reduction of alkyl esters of carbonic-carboxylic acid anhydrides at elevated temperature and pressure in the presence of platinum group metal catalysts, especially palladium on activated carbon, to make alcohols. Novel alkyl esters of carbonic-carboxylic acid anhydrides are disclosed, and can be used to make the corresponding alcohols, e.g., substituted benzyl alcohols. The alcohols can be converted to the corresponding halo, e.g., chloro, compounds. The substituted benzyl halides can be reacted with di(lower alkoxy)propionitriles, and the resulting 5-benzyl pyrimidines such as trimethoprim, 2,4-diamino-5-(3,4,5-trimethoxybenzyl)-pyrimidine, which is a known anti-bacterial agent, are especially useful in combination with sulfa drugs such as sulfamethoxazole. Other alcohols that can be made in accordance with the invention include 2,6-pyridine dimethanol which can be used to make pyridinol carbamate, an anti-inflammatory agent and an anti-arteriosclerotic agent and 1-aceto-4-hydroxymethyl-5-methyl imidazole, which can be converted into cimetidine.

Reduction of alkyl esters of carbonic-carboxylic anhydrides to alcohols

Compositions and a method for combatting cholera using novel substituted quinoxalines represented by the formula ##STR1## where R is hydrogen or lower alkyl of 1 to 5 carbon atoms, e.g., methyl to pentyl, are provided. A process for preparing the compounds is also provided.

Quinoxaline compound and composition, process for preparing compound,

A composition of cysteamine and a compound represented by the formula ##SPC1## Where R is hydrogen, --CHO or ##EQU1## useful for the treatment of an animal infected with a virus.

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Lodi, Italy

Andrea Bottazzi