Abstract: Crystalline form of abacavir that is essentially free of solvent of formula (I), in particular crystalline Form I, and its preparation process which comprises the following steps: a) crystallizing abacavir from a solution of said compound in a (C1-C4)-alcohol, dichloromethane, acetonitrile/water, or mixtures thereof; b) isolating the crystalline form of abacavir that appears in the prior step; and c) removing the solvent from the crystalline form of abacavir thus obtained. Crystalline Form I can also be obtained by dispersion of abacavir in acetonitrile. The crystalline form of abacavir that is essentially free of solvent is useful for the preparation of pharmaceutical compositions for use in the treatment and/or prophylaxis of HIV infections.

Abstract: The present invention relates to polymorphs and solvates of the hydrochloride salt of 4-[2-[[5-methyl-1-(2-naphthalenyl)-1H-pyrazol-3-yl]oxy]ethyl]morpholine (P027), processes for their preparation, and to pharmaceutical compositions comprising them.

Abstract: The invention relates to a process for preparing 1-aryl-pyrazol-3-one intermediates, tautomers, and salts thereof, to novel intermediates, and to the use of the intermediates in the preparation of sigma receptor inhibitors.

Abstract: A preparation process of esomeprazole sodium substantially free of sulfone impurity including the steps of: a) combining either esomeprazole with a (C3-C8)-ketone or a mixture thereof, a sodium alkoxide, and a (C1-C5)-alcohol, or esomeprazole sodium with a (C3-C8)-ketone or a mixture thereof and a (C1-C5)-alcohol; and b) recovering the esomeprazole sodium formed from the reaction media by filtration.

Abstract: It comprises a preparation process of entecavir comprising: submitting a (1S,3R)-3-(tert-butyldimethylsilyloxy)-1-(oxiran-2-yl)pent-4-yn-1-ol (VIII) to a double esterification and to a radicalary cyclization, yielding a compound of formula (V), where either a compound of formula (VIII) is submitted to a first esterification reaction, then to a catalytic radicalary cyclization using titanocene dichloride as catalyst in the presence of Mn/2,4,6-collidine HCl or Zn/2,4,6-collidine/trimethylsilyl chloride, and finally to a second esterification reaction or, alternatively, the compound of formula (VIII) is submitted first to a catalytic radicalary cyclization, and then to an esterification reaction. Entecavir can be obtained by submitting compound (V) to a desilylation reaction to remove the TBS group and then to a Mitsunobu coupling with 2-amino-6-chloroguanine, followed by hydrolysis. It also relates to some new intermediates of the process.

Abstract: The invention relates to a process for preparing 1-aryl-pyrazol-3-one intermediates, tautomers, and salts thereof, to novel intermediates, and to the use of the intermediates in the preparation of sigma receptor inhibitors.

Abstract: The present invention relates to polymorphs and solvates of the hydrochloride salt of 4-[2-[[5-methyl-1-(2-naphthalenyl)-1H-pyrazol-3-yl]oxy]ethyl]morpholine (P027), processes for their preparation, and to pharmaceutical compositions comprising them.

Abstract: A preparation process of esomeprazole sodium substantially free of sulfone impurity including the steps of: a) combining either esomeprazole with a (C3-C8)-ketone or a mixture thereof, a sodium alkoxide, and a (C1-C5)-alcohol, or esomeprazole sodium with a (C3-C8)-ketone or a mixture thereof and a (C1-C5)-alcohol; and b) recovering the esomeprazole sodium formed from the reaction media by filtration.

Abstract: Process for removal of the amino protective group of a N-acylated {(1S,4R)-4-[2-amino-6-(cyclopropylamino)-9H-purin-9-yl]-cyclopent-2-enyl}methanol of formula (II) where R?H or a (C1-C4)-alkyl, using an inorganic base in a mixture of water and alcohol, to yield abacavir or its salts. The process proceeds very fast and the product can be obtained in high yield and purity.

Abstract: Process for the preparation of abacavir, or its salts or its solvates comprising the step of reacting a compound (IV) where R1 is a (C1-C4)-alkyl radical with anhydrous hydrochloric acid/(C1-C6)-alcohol, and then with tri(C1-C4)-alkyl orthoformate, in the absence of water. The preparation process may include further steps of reacting the compound obtained with cyclopropylamine and subsequently hydrolysis to yield abacavir.

Abstract: New solid forms of the active ingredient magnesium salt of S-omeprazole, obtainable by a preparation process including: a) crystallizing a magnesium salt of S-omeprazole from a solution of a magnesium salt of S-omeprazole in a solvent system that includes a mixture of methanol/water with an amount of water equal to or greater than about 0.01 ml/g of the magnesium salt of S-omeprazole starting material; b) isolating the magnesium salt of S-omeprazole that appears in the prior operation; c) separating the free organic solvent from the magnesium salt of S-omeprazole obtained or, alternatively, separating both the free solvent and the solvation solvent. The new solid forms are obtained by a reproducible and robust process, with high yield and elevated optical purity, which is useful for the preparation of pharmaceutical products that contain said active ingredient.

Abstract: Crystalline form of abacavir that is essentially free of solvent of formula (I), in particular crystalline Form I, and its preparation process which comprises the following steps: a) crystallizing abacavir from a solution of said compound in a (C1-C4)-alcohol, dichloromethane, acetonitrile/water, or mixtures thereof; b) isolating the crystalline form of abacavir that appears in the prior step; and c) removing the solvent from the crystalline form of abacavir thus obtained. Crystalline Form I can also be obtained by dispersion of abacavir in acetonitrile. The crystalline form of abacavir that is essentially free of solvent is useful for the preparation of pharmaceutical compositions for use in the treatment and/or prophylaxis of HIV infections.

Abstract: Process for the preparation of optically active derivatives of 2-(2-piridylmethylsulfinyl)-benzimidazole, or salts thereof, by resolution of the corresponding racemic derivatives of 2-(2-piridylmethylsulfinyl)-benzimidazole. The resolution is performed through the formation of inclusion complexes with (S)-(?) or (R)-(+)-[1,1?-Binaphthalene]-2,2?-diol in the presence of an amine, followed by the break of the inclusion complex by treatment with an hydroxide of an alkaline metal. The enantiomer of the derivative of 2-(2-piridylmethylsulfinyl)-benzimidazole may be obtained by extractions at a particular pH with a suitable organic solvent. The process allows to perform the resolution with high yields and high optical purity, without using neither toxic solvents nor chromatography.

Abstract: An acetone solvate of phthaloyl amlodipine, as well as a process for its preparation including dissolving phthaloyl amlodipine in acetone and cooling the mixture. The present invention also comprises a method for the synthesis of amlodipine, its salts or solvates, which comprises the use of an acetone solvate of phthaloyl amlodipine.

Abstract: Process for the preparation of abacavir, or its salts or its solvates comprising the step of reacting a compound (IV) where R1 is a (C1-C4)-alkyl radical with anhydrous hydrochloric acid/(C1-C6)-alcohol, and then with tri(C1-C4)-alkyl orthoformate, in the absence of water. The preparation process may include further steps of reacting the compound obtained with cyclopropylamine and subsequently hydrolysis to yield abacavir.

Abstract: Process for removal of the amino protective group of a N-acylated [(1S,4R)-4-[2-amino-6-(cyclopropylamino)-9H-purin-9-yl]-cyclopent-2-enyl]methanol of formula (II) where R?H or a (C1-C4)-alkyl, using an inorganic base in a mixture of water and alcohol, to yield abacavir or its salts. The process proceeds very fast and the product can be obtained in high yield and purity.

Abstract: An acetone solvate of phthaloyl amlodipine, as well as a process for its preparation including dissolving phthaloyl amlodipine in acetone and cooling the mixture. The present invention also comprises a method for the synthesis of amlodipine, its salts or solvates, which comprises the use of an acetone solvate of phthaloyl amlodipine.

Abstract: Process for the preparation of optically active derivatives of 2-(2-piridylmethylsulfinyl)-benzimidazole, or salts thereof, by resolution of the corresponding racemic derivatives of 2-(2-piridylmethylsulfinyl)-benzimidazole. The resolution is performed through the formation of inclusion complexes with (S)-(?) or (R)-(+)-[1,1?-Binaphthalene]-2,2?-diol in the presence of an amine, followed by the break of the inclusion complex by treatment with an hydroxide of an alkaline metal. The enantiomer of the derivative of 2-(2-piridylmethylsulfinyl)-benzimidazole may be obtained by extractions at a particular pH with a suitable organic solvent. The process allows to perform the resolution with high yields and high optical purity, without using neither toxic solvents nor chromatography.

Abstract: New solid forms of the active ingredient magnesium salt of S-omeprazole, obtainable by a preparation process including: a) crystallizing a magnesium salt of S-omeprazole from a solution of a magnesium salt of S-omeprazole in a solvent system that includes a mixture of methanol/water with an amount of water equal to or greater than about 0.01 ml/g of the magnesium salt of S-omeprazole starting material; b) isolating the magnesium salt of S-omeprazole that appears in the prior operation; c) separating the free organic solvent from the magnesium salt of S-omeprazole obtained or, alternatively, separating both the free solvent and the solvation solvent. The new solid forms are obtained by a reproducible and robust process, with high yield and elevated optical purity, which is useful for the preparation of pharmaceutical products that contain said active ingredient.

Abstract: The present invention relates to polymorphs and solvates of the hydrochloride salt of 4-[2-[[5-methyl-1-(2-naphthalenyl)-1H-pyrazol-3-yl]oxy]ethyl]morpholine (P027), processes for their preparation, and to pharmaceutical compositions comprising them.