Inke, S.a.

Vita-invest S.a.

Laboratorios Lesvi, S.l.

Joan Huguet Clotet

Pere Dalmases Barjoan

Juan Carlos Del Castillo Nieto

Francisco Marquillas Olondriz

Marisabel Mourelle Mancini

Juan Antonio Perez Andres

Jose Maria Caldero Ges

Elisabet De Ramon Amat

Anna Bosch Rovira

Joan Maria Roca Acin

Ma Ángeles Conde Martínez

Sergio Rodríguez Ropero

Maria Chalaux Freixa

Jordi Bessa Belmunt

Juan Antonio Pérez Andrés

Javier Jesús Poza Soto

Sergio RODRÍGUEZ Ropero

Mª ÁNgeles Conde MARTÍNEZ

The present invention relates to an improved process for the preparation of 1-deoxy-1-methylamino-D-glucitol 2-(3,5-dichlorophenyl)-6-benzoxazolecarboxylate, also known as tafamidis meglumine. The process of the present invention is particularly suitable for industrial scale manufacture of tafamidis meglumine with excellent purity and high yields.

Process for preparing 1-deoxy-1-methylamino-d-glucitol 2-(3,5-dichlorophenyl)-6-benzoxazolecarboxylate

The present invention relates to an efficient and environmentally friendly process for preparing (3RS)-3-[(2SR)-(2-cyclopentyl-2-hydroxy-2-phenylacetyl)oxy]-1,1-dimethylpyrrolidinium bromide with high yield and purity suitable for industrial scale applications.

Process for preparing (3RS)-3-[(2SR)-(2-cyclopentyl-2-hydroxy-2-phenylacetyl)oxy]-1,1-dimethylpyrrolidinium bromide

The invention provides a method for obtaining the intermediate (II), useful for manufacturing Valsartan and a drug directed to a treatment of arterial hypertension or heart failure. The process comprises a) Imination of the aldehyde group of a compound (VII) by L-Valine (IV) salts with organic or inorganic bases and a polar solvent or water, where X means halogen or an &#x2014;OSO2R group, where R is CF3, tolyl, methyl or F; to give an imine-type compound (VIII), where B+ is the protonated form of an organic base or an alkaline cation; b) Reduction of the imine group of the compound (VIII) followed by acidification, to give the compound (VI); and c) N-Acylation of the compound (VI) with valeryl chloride to give the compound (II). Steps a) and b) can be performed in a 'one pot' reaction. 

Process for obtaining valine derivatives useful for obtaining a pharmaceutically active compound

The present invention relates to intermediates useful in the synthesis of Dolasetron and synthetic precursors thereof, as well as to processes for obtaining them. In addition, it refers to the hydrochloric salt of Dolasetron and polymorphic forms of Dolasetron and precursors thereof.

Intermediate compounds useful to prepare dolasetron

It is provided a method for obtaining Irbesartan polymorph A, with few synthesis steps, by coupling the intermediate of formula (II) with the compound of formula (III), neutralising one of its alkaline salts in an aqueous medium and recrystallising the crude product obtained. The utilisation of said method obviates protection and deprotection of the tetrazole ring and is therefore of considerable interest for obtaining Irbesartan on a large industrial scale. The invention also refers to the synthesis intermediate of formula (II). 

Method for obtaining a pharmaceutically active compound (Irbesartan) and its synthesis intermediate

This invention relates to a process for preparing intermediates useful in preparing Valsartan and to a process for preparing the latter, together with synthesis intermediates of formula (IV), (V) and (VI), useful for manufacturing a medicament for the treatment of arterial hypertension or heart failure. The process for preparing Valsartan permits it to be prepared on an industrial scale with high yields and without racemisation problems, in addition to using simple and available starting products. The invention also provides a process for preparing the intermediate of formula (VI), from an intermediate of formula (V) that does not require protection of the carboxylic acid prior to N-acylation. 

Process for the preparation of Valsartan and precursors thereof

New esters derived from substituted phenyl-cyclohexyl compounds, which are derived from Tramadol, process for obtaining them and their use for preparing a drug with analgesic properties. These new compounds of general formula (I) have a higher analgesic activity, a lower toxicity and a longer effective time period than Tramadol.

Esters derived from substituted phennyl-cyclohexyl compounds

Drug active on the central nervous system, a process for the preparation

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Sant Joan Despi, Spain

Joan Huguet Clotet