Sigma-tau Industrie Farmaceutiche Riunite S.p.a.

501 Sigma Tau Industrie Farmaceutiche Riunite S.p.a.

Carlo A Bagolini

Maria Ornella Tinti

Emma Quaresima

Carlo Scolastico

Domenico Misiti

Paolo DeWitt

Paolo De Witt

Mose Santaniello

Angelo De Luca

Agostino Uttaro

Silverio Fontana

An improved process is described for the industrial preparation of L-carnitine or alkanoyl L-carnitine mucate, which allows operations in a homogeneous phase in conditions of greater dilution, in a normal chemical reactor with stirring, in a batch process.

Process for the preparation of salts of L-carnitine and alkanoyl L-carnitine with mucic acid

A process for making valproic acid from an alkyl alkanoylacetate is disclosed. The alkyl alkanoylacetate is reacted with an n-propyl halide in a biphasic system in the presence of a base and a phase transfer catalyst. The product mixture is acidified to convert the resulting valproate salt into valproic acid.

Process for producing valproic acid

L-aminoacyl derivatives of L-carnitine of general formula (I) ##STR1## wherein R is an alkyl radical selected from 1-methyl-propyl, isobutyl, isopropyl, mercaptomethyl and 3-guanidino propyl, and their pharmacologically acceptable salts, are prepared e.g. by reacting a solution in an organic solvent of L-carnitine whose carboxyl group is protected with an N-protected aminoacid in the presence of a condensing agent and then removing the amino-acid and carnitine protecting groups, thus obtaining the desired compound.

Derivatives of L-amino acyl L-carnitine, process for their preparation

L-aminoacyl derivatives of L-carnitine of general formula (I) ##STR1## wherein R is an alkyl radical selected from 1-methyl-propyl, isobutyl, isopropyl, mercaptomethyl and 3-guanidino propyl, and their pharmacologically acceptable salts, are prepared e.g. by reacting a solution in an organic solvent of L-carnitine whose carboxyl group is protected with an N-protected aminoacid in the presence of a condensing agent and then removing the aminoacid and carnitine protecting groups, thus obtaining the desired compound.

A novel class of mercapto acyl-carnitines is disclosed, wherein the mercapto acyl radical is the radical of saturated mercapto acids having from 2 to 10 carbon atoms. These mercapto acyl-carnitines are prepared, e.g., by first preparing the corresponding halogen acyl-carnitine and then substituting therein, by nucleophylic substitution, the --SH group for the halogen atom. These mercapto acyl-carnitines are useful therapeutic agents, e.g., for the treatment of intoxications and burns and as mucolytic agents. Dithio diacyl carnitines and hydrochloride salts thereof, which are intermediates, are also disclosed.

Mercapto acyl-carnitines and pharmaceutical compositions containing same

A novel class of esters of mercapto acyl-carnitines is disclosed, wherein the mercapto acyl radical is the radical of saturated mercapto acids having from 2 to 10 carbon atoms. These esters of mercapto acyl-carnitines are prepared e.g. by first preparing the corresponding ester of halogen acyl-carnitine and then substituting therein, by nucleophylic substitution, the --SH group for the halogen atom. These esters of mercapto acyl-carnitines are useful therapeutic agents, e.g. for the treatment of intoxications and burns, and as mucolytic agents.

Esters of mercapto acyl-carnitines and pharmaceutical compositions

Dithiodiacyl carnitines, intermediates for the preparation of mercaptoacyl-carnitines, are disclosed. These mercapto acyl-carnitines are useful therapeutic agents, e.g. for the treatment of intoxications and burns and as mucolytic agents.

Growing community of inventors

Rome, Italy

Carlo A Bagolini