Politechnika Gdanska

Elzbieta Troka

Edward Borowski

Leonard S Falkowski

Barbara J Stefanska

Jerzy J Golik

Andrzej B Jarzebski

Jan Zielinski

Pawel Kolodziejczyk

Emilia Cybulska

The invention relates to amides of polyene macrolide antibiotics and their derivatives characterized by the general formula I, ##STR1## where R is the polyene macrolide, R.sub.1 is an alkyl or isoalkyl chain of from one to eighteen carbons, unsubstituted or substituted with a primary or secondary amine; where R.sub.2 is an hydrogen or R.sub.1 or R.sub.1 and R.sub.2 are joined through the nitrogen to form a heterocyclic ring. The method of preparation of these substances according to our invention depends upon the reaction of the polyene macrolide or its derivative in which the carboxylic group is activated; in the environment of an organic solvent or mixture of solvents and in the presence of a substance neutralizing the acid; with a compound containing an amino group; leaving upon completion of the reaction; and precipitation of the product from the reaction mixture, by addition of ethyl ether or a mixture of ethyl ether with hydrocarbons; isolation and purification of the product by means of known methods.

Amides of amphoteric polyene macrolide antibiotics

A process for production of esters of antibiotics from the group of polyene macrolides and of N-substituted derivatives thereof, having the general Formula 1, wherein R denotes the radical of antibiotic or of its R-COOR, I N-substituted derivative, and R.sub.1 denotes an alkyl with the chain length of C.sub.1 through C.sub.5, or an aryl, consisting therein that an antibiotic from the group of polyene macrolides or its N-substituted derivative is dissolved or suspended in alcohol and/or neutral organic solvent, or in a mixture of organic solvents, in presence of dicyclohexylcarbodiimide and/or hydrocybenzotriazole, the whole is allowed to stand at room temperature, or at temperature elevated to 40.degree. C., and then the obtained product is isolated from the reaction medium after known methods.

Method of preparation of esters of antibiotics selected from the group

Inorganic salts of trimethylammonium derivatives of polyene macrolides, particularly the inorganic salts of methyl esters of these derivatives having the general formula: ##STR1## wherein R is the residue of a polyene macrolide and X is an anion of a salt selected from the group consisting of methylsulphate, sulphate, chloride, phosphate and acetate. The preparation of salts of formula (I) or formula (II) is also disclosed.

Water-soluble salts of trimethylammonium derivatives of polyene

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Gdansk-Oliwa, Poland

Elzbieta Troka