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

Roberto Castagnani

Paolo De Witt

Oreste Piccolo

Maria Ornella Tinti

Fabio Giannessi

Domenico Misiti

Francesco De Angelis

Walter Cabri

Silvia Armaroli

Gianandrea Quattrociocchi

Vincenzo Colangeli

Oreste Piccoloi

Paolo De Witt Scalfaro

The present invention provides a new process of synthesis of a polymorph of 7-chloro-4-(piperazin-1-yl)-quinoline of Formula I. Said quinoline compound is substantially pure of any impurities. The present invention further provides the use of the above-mentioned polymorph of 7-chloro-4-(piperazin-1-yl)-quinoline in the synthesis of piperaquine or one of its pharmaceutically acceptable salts. 

Process for the synthesis of 7-chloro-4-(piperazin-1-yl)-quinoline

A process for the production of (R)- or (S)-aminocarnitine starting respectively from (R)- or (S)-nitryloxycarnitine, through the formation and hydrogenation of the azidocarnitine intermediate with the same absolute configuration is described. (R)-aminocarnitine inner salt is obtained after purification, which is then converted into non-deliquescent salts. Also a process for the preparation of derivatives of (R)- and (S)-aminocarnitine, in particular acylayed or ureic derivatives, having known pharmacological properties, starting from (R)- and (S)-aminocarnitine salts, releasing the aminic function in situ.

Process for the preparation of (r)- or (s)-aminocarnitine inner salt, the salts and derivatives thereof

A new, more efficient and highly stereospecific process is described for the preparation of compounds with general formula (R)-(I) and of absolute configuration (R), where the groups M, W, Q and Q are as defined in the description, starting from compounds of absolute configuration (S) by hydrolysis, in the presence of acids, of the corresponding esterified derivatives. The (R)-(I) products obtained with the process described herein are chiral synthons useful for the production of enanthiomerically pure drugs. The preparation of (R)-carnitine is also provided.

Stereospecific hydrolysis of optically active esters

Nitriloxy derivatives of (R) and (S)-carnitine

A process for producing aminocarnitine is described, wherein methanesulfonylcarnitine is converted to a lactone which is reacted with an azide to give azidocarnitine. The catalytic hydrogenation of azidocarnitine gives aminocarnitine.

Process for producing R-aminocarnitine and S-aminocarnitine

A Process for Preparing L-(-)-carnitine is disclosed which comprises acylating D-(+)-carnitinenitrile or D-(+)-carnitineamide to their respective acyl derivatives which, via acid hydrolysis, yield D-(+)-carnitine which is converted to the lactone of L-(-)-carnitine. The lactone when in base yields L-(-)-carnitine.

Process for manufacturing L-(-)-carnitine from derivatives having a

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Recanati, Italy

Roberto Castagnani