Interquim, S.a.

Marta Pomares Marco

Francisco Marquillas Olondriz

Francisco De Asís Marquillas Olondriz

Antonio Abelino De León Martín

Santos Hernàndez Gallego

Jorge Bessa Bellmunt

It is provided a process for the preparation of aripiprazole lauroxil that comprises reacting 1-(hydroxymethyl) aripiprazole with lauric anhydride in the presence of DMAP and a solvent.

Process for the preparation of aripiprazole lauroxil

It is provided a process for the preparation of aripiprazole lauroxil that comprises reacting 1-(hydroxymethyl) aripiprazole with lauric acid in the presence of a suitable solvent and a carboxyl activating agent in the presence of a suitable solvent and, optionally, in the presence of an appropriate base. 1-(Hydroxymethyl) aripiprazole can be prepared by reacting aripiprazol or an hydrate thereof with paraformaldehyde in the presence of a suitable organic solvent and a suitable base, wherein the reaction is carried out without the addition of water as a solvent to the reaction mixture. Additionally, (7-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butoxy)-3,4-dihydro-2-oxoquinolin-1(2H)-yl)methyl formate is provided as a reference standard.

The present invention relates to new processes for the preparation of synthesis intermediate products useful in the preparation of Dabigatran Etexilate on an industrial scale. The invention also relates to new crystalline forms of intermediate products thus obtained.

Process for the preparation of intermediates for the synthesis of Dabigatran Etexilate, and crystalline forms of said intermediates

The present invention describes a novel process for the preparation of optically active (S)-(&#x2212;)-2-(N-propylamino)-5-methoxytetraline and (S)-(&#x2212;)-2-(N-propylamino)-5-hydroxytetraline compounds based on the optical resolution of mixtures of the enantiomers of 2-(N-propylamino)-5-methoxytetraline and 2-(N-propylamino)-5-hydroxytetraline respectively. This process comprises (a) reacting a mixture of the enantiomers of said compounds with an optically active organic acid to form diastereoisomeric salts and separating the salts by crystallization. Said compounds are useful in the preparation of (6S)-(&#x2212;)-5,6,7,8-tetrahydro-6-[propyl-(2-thienyl)ethyl]amino-1-naphthol (Rotigotine). Rotigotine is a dopamine agonist and is indicated for the treatment of Parkinson's disease.

Process for the preparation of optically active (S)-(&#x2212;)-2-(N-propylamino)-5-methoxytetraline and (S)-(&#x2212;)-2-(N-propylamino)-5-hydroxytetraline compounds

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Marta Pomares Marco