Inke, S.a.

Laboratorios Lesvi, S.l.

Vita Cientifica, S.a.

Jordi Bessa Bellmunt

Pere Dalmases Barjoan

Juan Huguet Clotet

Glòria Freixas Pascual

Lluis Sola Carandell

Jordi Carles Ceron Bertran

Jordi Cerón Bertran

Antonio Abelino De Leon Martin

Lluís Sola Carandell

Antonio Abelino De León Martín

The present invention refers to an improved method for the preparation of compound 1-(2,6-difluorobenzyl)-1H-1,2,3-triazole-4-carboxylic acid substantially free of its 3H-I isomer. The invention also refers to the use of said intermediate for the preparation of Rufinamide and for obtaining a new polymorphic form of Rufinamide, designed as Form R-5. The invention also refers to said new polymorph of Rufinamide, and to the composition containing it and its use as medicament. The new polymorph of Rufinamide shows good stability and appropriate physico-chemical properties for its manipulation on industrial scale. Polymorph Form R-5 will be suitable to use as pharmaceutical for the treatment of convulsions, especially for the treatment of epilepsy.

Process for preparing rufinamide intermediate

Said mixed solvate is a solvate of olanzapine/water/tetrahydrofuran in the proportion 1:1:1/2 (I). The method for preparing said solvate comprises treating a crude anhydrous olanzapine with a mixture of tetrahydrofuran/water. The method for preparing Form I of olanzapine includes desolvating the mixed solvate of formula I, by means of drying, in vacuo and under temperature-controlled conditions. 

Mixed solvate of olanzapine, method for preparing it and method for preparing form I of olanzapine therefrom

The invention discloses a method for preparing the intermediate 2-(2,3-dichlorophenyl)-2-(aminoguanidine)acetonitrile of formula (II), which comprises the reaction of 2,3-dichlorobenzoyl cyanide with aminoguanidine bicarbonate in non-aqueous medium in the presence of methanesulphonic acid, which produces good yields and short reaction times. Said intermediate is useful for preparing 3,5-diamino-6-(2,3-dichlorophenyl)-1,2,4-triazine of formula (I). The invention also relates to a method for preparing (I) with high purity 

Process for preparing a pharmaceutically active compound and for preparing its intermediate

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Barcelona, Spain

Jordi Bessa Bellmunt