Abstract: The invention relates to the production of zinc trisodium pentetic acid (Zn-DTPA) and to new crystalline forms of said salt.

Abstract: The invention relates to a compound which is, 2-[4-[(methylamino)carbonyl]-1H-pyrazol-1-yl]adenosine, which is a selective A2A adenosine receptor agonist in myocardial imaging. The new polymorph of 2-[4-[(methylamino)carbonyl]-1H-pyrazol-1-yl]adenosine (designated as polymorph E) is characterized by an X-ray diffraction pattern of X-RPD showing the following reflections at 2 Theta=5.8°, 12.3°, 15.9°, 17.3°, 20.5°, 22.6°, 23.6°, 27.7°, and 29.2°; and further characterized by a DSC scan showing marked endotherm in the range of 258 to 264° C.; and further characterized by a specific IR spectra.

Abstract: A method of preparation of N-(1-benzo[b]thien-2-ylethyl)-N-hydroxyurea of formula (I) with the use of a reaction of 1-(benzo[b]thien-2-yl)-ethanol of formula (II) with hydroxyurea of formula (III) in organic solvents, organic acids, their mixtures or in mixtures thereof with water, being catalyzed by strongly acidic cation exchangers or various hydrogen sulphates.

Abstract: A new polymorph of 2-[4-[(methylamino)carbonyl]-1H-pyrazol-1-yl]adenosine (designated as polymorph E), characterized by an X-ray diffraction pattern of X-RPD showing the following reflections at 2 Theta=5.8°, 12.3°, 15.9°, 17.3°, 20.5°, 22.6°, 23.6°, 27.7°, and 29.2°, and further characterized by DSC showing marked endotherm in the range of 258 to 264° C.

Abstract: A method for the preparation of 2-(4-methoxycarbonylpyrazol-1-yl)adenosine of formula 1a and 2-(4-ethoxycarbonylpyrazol-1-yl)adenosine of formula 1b by reaction of 2-hydrazinoadenosine of formula III and the sodium salt of 3,3-dimethoxy-2-methoxycarbonylpropen-1-ol of formula Va or the sodium salt of 3,3-diethoxy-2-ethoxycarbonylpropen-1-ol of formula Vb in combination with a solvent and an acidic agent.

Abstract: A method for the preparation of 2-[4-[(methylamino)carbonyl]-1-H-pyrazol-1-yl]adenosine monohydrate of formula I by reaction of 2-(4-methoxycarbonylpyrazol-1-yl) adenosine of formula III with a solution of methylamine in a non-aqueous solvent, optionally in combination with another inert solvent, to produce anhydrous 2-[4-[(methylamino)carbonyl]-1-H-pyrazol-1-yl]adenosine, which is converted to 2-[4-[(methylamino)carbonyl]-1-H-pyrazol-1-yljadenosine monohydrate of formula I by addition of water.

Abstract: The invention deals with a preparation method of salts of 5-chloro-4-(2-imidazolin-2-yl-amino)-2,1,3-benzothiadiazole (tizanidine) of formula I, especially tizanidine hydrochloride, comprising preparation of a salt of tizanidine of formula I and a carboxylic acid as an intermediate, from which, after acidification with hydrogen chloride, tizanidine hydrochloride is obtained in a high yield and purity.

Abstract: Derivatives of 2-phenyl-3-hydroxyquinoline-4(1H)-one of the general formula (II), where X represents a nitro group, amino group, and Y represents an atom of halogen, oxygen or sulphur substituted by C1 to C6 alkyl or phenyl group, whereby both the alkyl and phenyl group may be further substituted and the substituents may be identical or different, or by nitrogen substituted independently by hydrogen, C1 to C6 alkyl, C1 to C6 alkyl, which may be substituted among others by halogen, hydroxy, C1 to C4 alkoxy or C1 to C4 alkylamino group, or may form a saturated or unsaturated heterocyclic ring with 5 to 7 atoms, where the individual ring atoms comprise atoms of carbon, and any of the carbon atoms may be substituted by an atom of nitrogen, sulphur or oxygen, X and Y together form an imidazo group, or imidazo group substituted by C1 to C6 alkyl, which may be substituted among others by halogen, hydroxy, C1 to C4 alkoxy or C1 to C4 alkylamino group, CHO or acetylgroup, or a heterocyclic ring with 5 to 6 atoms, wher

Abstract: A method for preparing 4-[3,5-bis(2-hydroxyphenyl )-[1,2,4]triazol-1-yl]benzoic acid of formula (I) by reaction of 2-(2-hydroxyphenyl)benz[e][1,3]oxazin-4-one of formula (II) with 4-hydrazinobenzoic acid of formula (III) in an organic acid or in a mixture of an organic acid and an organic solvent.

Abstract: The invention deals with a preparation method of salts of 5-chloro-4-(2-imidazolin-2-yl-amino)-2,1,3-benzothiadiazole (tizanidine) of formula I, especially tizanidine hydrochloride, comprising preparation of a salt of tizanidine of formula I and a carboxylic acid as an intermediate, from which, after acidification with hydrogen chloride, tizanidine hydrochloride is obtained in a high yield and purity.

Abstract: A method for the preparation of salts of 2-[2-(4-dibenzo[b,fj[1,4]thiazepin-11-yl-1 -piperazinyl)ethoxy]ethanol (quetiapine) from the quetiapine base and the respective acid, wherein the salt is precipitated from a mixture of solvents, the mixture being either a mixture of an aromatic hydrocarbon and a ketone or ester, or that of an aromatic hydrocarbon, water and a ketone or ester. The salts of quetiapine are purified by partial crystallization, wherein only a part of the salt of quetiapine is dissolved in a C1 to C6 alcohol used.

Abstract: A method of preparation of N-(1-benzo[b]thien-2-ylethyl)-N-hydroxyurea of formula (I) with the use of a reaction of 1-(benzo[b]thien-2-yl)-ethanol of formula (II) with hydroxyurea of formula (III) in organic solvents, organic acids, their mixtures or in mixtures thereof with water, being catalyzed by strongly acidic cation exchangers or various hydrogen sulphates.

Abstract: A method for preparing 4-[3,5-bis(2-hydroxyphenyl)-[1,2,4]triazol-1-yl]benzoic acid of formula (I) by reaction of 2-(2-hydroxyphenyl)benz[e][1,3]oxazin-4-one of formula (II) with 4-hydrazinobenzoic acid of formula (III) in an organic acid or in a mixture of an organic acid and an organic solvent.

Abstract: Derivatives of 2-phenyl-3-hydroxyquinoline-4(1H)-one of the general formula (II), where X represents a nitro group, amino group, and Y represents an atom of halogen, oxygen or sulphur substituted by C1 to C6 alkyl or phenyl group, whereby both the alkyl and phenyl group may be further substituted and the substituents may be identical or different, or by nitrogen substituted independently by hydrogen, C1 to C6 alkyl, C1 to C6 alkyl, which may be substituted among others by halogen, hydroxy, C1 to C4 alkoxy or C1 to C4 alkylamino group, or may form a saturated or unsaturated heterocyclic ring with 5 to 7 atoms, where the individual ring atoms comprise atoms of carbon, and any of the carbon atoms may be substituted by an atom of nitrogen, sulphur or oxygen, X and Y together form an imidazo group, or imidazo group substituted by C1 to C6 alkyl, which may be substituted among others by halogen, hydroxy, C1 to C4 alkoxy or C1 to C4 alkylamino group, CHO or acetylgroup, or a heterocyclic ring with 5 to 6 atoms, wher

Abstract: A method for the preparation of salts of 2-[2-(4-dibenzo[b,fj[1,4]thiazepin-11-yl-1-piperazinyl)ethoxy]ethanol (quetiapine) from the quetiapine base and the respective acid, wherein the salt is precipitated from a mixture of solvents, the mixture being either a mixture of an aromatic hydrocarbon and a ketone or ester, or that of an aromatic hydrocarbon, water and a ketone or ester. The salts of quetiapine are purified by partial crystallization, wherein only a part of the salt of quetiapine is dissolved in a C1 to C6 alcohol used.

Abstract: A process for preparing optically pure enantiomers of R-(?)tamsulosin of formula Ia and S-(+)tamsulosin of formula Ib by resolving racemic tamsulosin of formula I by means of (1R)-(?)-camphor-10-sulfonic acid and (1S)-(+)-camphor-10-sulfonic acid, resp., in an environment of organic solvents, water or mixtures thereof.

Abstract: A process for preparing optically pure enantiomers of R-(?)tamsulosin of formiula Ia and S-(+)tamsulosin of formula Ib by resolving racemic tamsulosin of formula I by means of (IR)-(?)-camphor-10-sulfonic acid and (1S)-(+)-camphor-10-sulfonic acid, resp., in an environment of organic solvents, water or mixtures thereof.