Recordati Industria Chimica E Farmaceutica S.p.a.

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

Cristina Crescenzi

Fausto Bonifacio

Maria Donnarumma

Dimitri Ippoliti

Maria Ornella Tinti

Sergio Penco

Oreste Piccolo

This invention relates to crystalline polymorphs of sertraline hydrocloride, i.e. (1S-cis)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-1-naphtalenamine hydrochloride, denominated form I, II and V, and methods for their preparation.

Methods for preparing sertraline hydrochloride polymorphs

This invention relates to a method for the preparation of sertraline hydrochloride, (1S-cis)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-1-naphtalenamine hydrochloride, in its crystalline form II.

Sertraline hydrochloride form II and methods for the preparation thereof

The present invention describes a process for the industrial production of L-carnitine, comprising the enantioselective reduction of an alkyl 4-chloro-3-oxobutyrate or 4-chloro-3-oxobutyramide. The optically active 3-hydroxy derivative thus obtained is reacted with trimethylamine, obtaining crude L-carnitine, which is then finally purified. The catalyst used for the reduction is a complex of ruthenium bound to a penta-atomic bis-heteroaromatic system. The reduction reaction, performed in controlled conditions of hydrogen pressure, substrate concentration, temperature, and substrate: catalyst molar ratio, enables 4-chloro-3-hydoxybutyrate or 4-chloro-hydroxybutyamide to be obtained in a high yield. The process described, which leads to L-carnitine being obtained, is easily applicable on an industrial scale.

Industrial process for the production of L-carnitine

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Rome, Italy

Cristina Crescenzi