Abstract: It is provided a method for the purification of vilanterol trifenatate of formula (I) comprising crystallizing vilanterol trifenatate from a ketone solvent selected from the group consisting of methyl ethyl ketone (MEK), methyl isobutyl ketone (MIK), ethyl isopropyl ketone, methyl isopropyl ketone, 3-methyl-2-pentanone, and a mixture thereof.

Abstract: The present invention provides a new process for stabilizing the particle size of micronized glycopyrronium salt (such as glycopyrronium bromide) which yields a micronized product exhibiting improved chemical and polymorphic stability even after prolonged storage. The invention also relates to compositions comprising said stabilized glycopyrronium salt (such as glycopyrronium bromide) and to dry powder inhaler devices and capsules or blisters comprising the stabilized glycopyrronium salt (such as glycopyrronium bromide). The glycopyrronium salt (such as glycopyrronium bromide) or compositions of the invention may be used as a medicament, for instance in the treatment of asthma, chronic obstructive pulmonary disease or cystic fibrosis or related diseases.

Abstract: The present invention provides an improved process for the manufacture (R)-6-hydroxy-8-[1-hydroxy-2-[2-(4-methoxyphenyl)-1,1-dimethyl-ethylamino-ethyl]-2H-1,4-benzoxazin-3(4H)-one, in high purity and high yield, through the use of 1,1-dimethyl-2-(4-methoxyphenyl)ethyl amine L-tartrate salt, 1,1-dimethyl-2-(4-methoxyphenyl)ethyl amine maletate salt or the camphorsulfonate salt of intermediate (4). The invention also relates to said salts, to processes for preparing them and to their use for the manufacture of (R)-6-hydroxy-8-[1-hydroxy-2-[2-(4-methoxyphenyl)-1,1-dimethyl-ethylamino-ethyl]-2H-1,4-benzoxazin-3(4H)-one or a pharmaceutically acceptable salt thereof.

Abstract: The present invention relates to an improved process for obtaining Paliperidone, I, comprising alkylating compound VI, or a salt thereof, with compound V, or a salt thereof, using a base selected from triethylamine or diisopropylethylamine and, optionally, a solvent. Moreover, the invention relies on the preparation of intermediates used in such process.

Abstract: Relates to a new polymorphic form of Granisetron base, Form I, to methods for obtaining thereof, to the method for obtaining Granisetron.HCl and its use for preparing pharmaceutical formulations. The Form I is characterized by the X-ray powder diffractogram shown in FIG. 1. Included in summarised form are the methods and solvents for obtaining the Form I: 1) Evaporation of hexane at atmospheric pressure; 2) Evaporation of acetone at atmospheric pressure; 3) Evaporation of toluene at atmospheric pressure; 4) Cooling of a saturated solution of diethyl ether to reflux temperature; 5) Evaporation of 2-propanol atmospheric pressure; 6) Evaporation of tetrahydrofuran at atmospheric pressure; and 7) Cooling of a saturated solution of acetonitrile to reflux temperature.

Abstract: An improved method is provided for preparing a mixed solvate of olanzapine/water/tetrahydrofuran in a proportion of 1:1:1/2. Said improvement is characterised in that said mixed solvate is basically prepared by means of methylation of the N-desmethylolanzapine with dimethyl sulphate, using tetrahydrofuran and water as solvents.

Abstract: 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 —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.

Abstract: 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.

Abstract: The invention relates to a procedure for preparing quetiapine by reaction between a compound of formula (II) and a compound of formula (III), in which X means a leaving group and P a protective group of alcohols resistant to alkaline conditions, in the presence of a base, followed by a step of deprotection and, optionally, obtaining a pharmaceutically acceptable salt thereof. Said procedure permits the obtaining of quetiapine with a high degree of purity under soft temperature conditions, with short reaction times and avoiding the use of toxic solvents.

Abstract: 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 —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.

Abstract: Relates to a new polymorphic form of Granisetron base, Form I, to methods for obtaining thereof, to the method for obtaining Granisetron.HCl and its use for preparing pharmaceutical formulations. The Form I is characterized by the X-ray powder diffractogram shown in FIG. 1. Included in summarised form are the methods and solvents for obtaining the Form I: 1) Evaporation of hexane at atmospheric pressure; 2) Evaporation of acetone at atmospheric pressure; 3) Evaporation of toluene at atmospheric pressure; 4) Cooling of a saturated solution of diethyl ether to reflux temperature; 5) Evaporation of 2-propanol atmospheric pressure; 6) Evaporation of tetrahydrofuran at atmospheric pressure; and 7) Cooling of a saturated solution of acetonitrile to reflux temperature.

Abstract: 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.

Abstract: The present invention relates to a method for obtaining Dolasetron that comprises: a) Esterification of the alcohol of formula (IV) with indole-3-carboxylic acid (compound (III)) or a reactive derivative thereof, to give a compound of formula (V), followed by step b) which includes Dieckmann reaction of the intermediate (V), by reaction with a strong organic or inorganic base, to give the intermediate (VI), and step c) which comprises dealcoxycarbonylation of the intermediate (VI) to give Dolasetron base and, if desired, a pharmaceutically acceptable salt thereof, hydrates or solvates of the base of said salt. The invention also relates to the intermediates (V) and (VI), and methods for obtaining them. With the method of the present invention Dolasetron is obtained at industrial scale with good yields, with decreased use of reactants and solvents, while said method is also of greater atomic efficiency.

Abstract: 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).

Abstract: 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.

Abstract: An improved method is provided for preparing a mixed solvate of olanzapine/water/tetrahydrofuran in a proportion of 1:1:1/2. Said improvement is characterised in that said mixed solvate is basically prepared by means of methylation of the N-desmethylolanzapine with dimethyl sulphate, using tetrahydrofuran and water as solvents.

Abstract: In particular, this invention relates to the synthesis intermediates (IV), (V), (VI) and (VIII) useful for preparing zolmitriptanzohnitriptan or a pharmaceutically acceptable salt thereof, which includes a) Ppreparation of the diazonium salt of the aniline hydrochloride (II); followed by reduction and acidification to give hydrazine (III); b) In situ Reaction of the hydrazine hydrochloride (III) with ?-keto-?-valerolactone, to give the hydrazone (IV); c) Fischer indole synthesis of the hydrazone (IV), to give the pyranoindolone of formula (V); d) Ttransesterification of the pyranoindolone (V) to provide the compound (VI), in which R means a straight or branched C1-C4 alkyl; e) Conversion of the hydroxyl group of the compound (VI) into dimethylamino to give the indolecarboxylate (VII), in which R means a straight or branched C1-C4 alkyl; f) Ssaponification of the 2-carboalkoxy group of the compound (VII), to provide indolecarboxylic acid (VIII); g) Ddecarboxylation of the indolecarboxylic acid (VIII), to provi

Abstract: 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).

Abstract: In particular, this invention relates to the synthesis intermediates (IV), (V), (VI) and (VIII) useful for preparing zolmitriptanzohnitriptan or a pharmaceutically acceptable salt thereof, which includes a) Preparation of the diazonium salt of the aniline hydrochloride (II); followed by reduction and acidification to give hydrazine (III); b) In situ Reaction of the hydrazine hydrochloride (III) with ?-keto-?-valerolactone, to give the hydrazone (IV); c) Fischer indole synthesis of the hydrazone (IV), to give the pyranoindolone of formula (V); d) Transesterification of the pyranoindolone (V) to provide the compound (VI), in which R means a straight or branched C1-C4 alkyl; e) Conversion of the hydroxyl group of the compound (VI) into dimethylamino to give the indolecarboxylate (VII), in which R means a straight or branched C1-C4 alkyl; f) Saponification of the 2-carboalkoxy group of the compound (VII), to provide indolecarboxylic acid (VIII); g) Decarboxylation of the indolecarboxylic acid (VIII), to provide z

Abstract: 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.