Abstract: The present invention provides a manufacturing process for preparing a peptide, preferably a decapeptide, such as degarelix, by incorporating p-nitro-phenylalanin in the amino acid sequence preferably during stepwise solid phase synthesis, and converting these into the required amino acids Aph(Hor) and/or D-Aph(Cbm), preferably while attached to a solid phase. The invention further provides intermediates useful in the manufacturing process.

Abstract: The present invention provides a manufacturing process for preparing a peptide, preferably a decapeptide, such as degarelix, by incorporating p-nitro-phenylalanin in the amino acid sequence preferably during stepwise solid phase synthesis, and converting these into the required amino acids Aph(Hor) and/or D-Aph(Cbm), preferably while attached to a solid phase. The invention further provides intermediates useful in the manufacturing process.

Abstract: The present invention provides a manufacturing process for preparing a peptide, preferably a decapeptide, such as degarelix, by incorporating p-nitro-phenylalanin in the amino acid sequence preferably during stepwise solid phase synthesis, and converting these into the required amino acids Aph(Hor) and/or D-Aph(Cbm), preferably while attached to a solid phase. The invention further provides intermediates useful in the manufacturing process.

Abstract: The present application provides an improved process for the preparation of sugammadex by reacting a salt of 3-mercapto propionic acid with 6-per-deoxy-6-per-halo-?-cyclodextrin in a suitable organic solvent. This application also provides crystalline form of a salt of 3-mercapto propionic acid, preferably di sodium salt of 3-mercapto propionic acid and its use for the preparation of sugammadex, whereas formula (I) shows the sodium salt of sugammadex.

Abstract: The present application provides an improved process for the preparation of sugammadex by reacting a salt of 3-mercapto propionic acid with 6-per-deoxy-6-per-halo-?-cyclodextrin in a suitable organic solvent. This application also provides crystalline form of a salt of 3-mercapto propionic acid, preferably di sodium salt of 3-mercapto propionic acid and its use for the preparation of sugammadex, whereas formula (I) shows the sodium salt of sugammadex.

Abstract: The present application provides crystalline forms of 6-per-deoxy-6-per-chloro-?-cyclodextrin, and polymorphs thereof. The present application also provides methods for preparing said polymorphs by dissolving 6-per-deoxy-6-per-chloro-?-cyclodextrin in dimethylformamide and using an anti-solvent of a water/alcohol mixture.

Abstract: The present application provides an improved process for the preparation of sugammadex which comprises the halogenation of ?-cyclodextrin in a suitable organic solvent to give 6-per-deoxy-6-per-halo-?-cyclodextrin, wherein halo is bromo or chloro, reacting the halogenated ?-cyclodextrin with 3-mercaptopropionic acid in the presence of alkoxide base to obtain sugammadex of formula I. This application also provides isolation of 6-per-deoxy-6-per-chloro-?-cyclodextrin as a crystalline compound and its use for the preparation of sugammadex of formula (I).

Abstract: The present invention provides a manufacturing process for preparing a peptide, preferably a decapeptide, such as degarelix, by incorporating p-nitro-phenylalanin in the amino acid sequence preferably during stepwise solid phase synthesis, and converting these into the required amino acids Aph(Hor) and/or D-Aph(Cbm), preferably while attached to a solid phase. The invention further provides intermediates useful in the manufacturing process.

Abstract: The present application provides an improved process for the preparation of sugammadex which comprises the halogenation of ?-cyclodextrin in a suitable organic solvent to give 6-per-deoxy-6-per-halo-?-cyclodextrin, wherein halo is bromo or chloro, reacting the halogenated ?-cyclodextrin with 3-mercaptopropionic acid in the presence of alkoxide base to obtain sugammadex of formula I. This application also provides isolation of 6-per-deoxy-6-per-chloro-?-cyclodextrin as a crystalline compound and its use for the preparation of sugammadex of formula (I).

Abstract: The present application provides crystalline forms of 6-per-deoxy-6-per-chloro-?-cyclodextrin, and polymorphs thereof. The present application also provides methods for preparing said polymorphs by dissolving 6-per-deoxy-6-per-chloro-?-cyclodextrin in dimethylformamide and using an anti-solvent of a water/alcohol mixture.

Abstract: The present invention is directed to (?)-(2R,3S)-2-amino-3-hydroxy-3-pyridin-4-yl-1-pyrrolidin-1-yl-propan-1-one (L)-(+) tartrate salt, a pharmaceutical composition comprising said salt, a process for making said salt, and the use of said salt in the treatment of pain.

Abstract: The present invention is directed to (?)-(2R,3S)-2-amino-3-hydroxy-3-pyridin-4-yl-1-pyrrolidin-1-yl-propan-1-one (L)-(+) tartrate salt, a pharmaceutical composition comprising said salt, a process for making said salt, and the use of said salt in the treatment of pain.

Abstract: The present invention is directed to (?)-(2R,3S)-2-amino-3-hydroxy-3-pyridin-4-yl-1-pyrrolidin-1-yl-propan-1-one (L)-(+)tartrate salt, a pharmaceutical composition comprising said salt, a process for making said salt, and the use of said salt in the treatment of pain.

Abstract: The present invention is directed to (?)-(2R,3S)-2-amino-3-hydroxy-3-pyridin-4-yl-1-pyrrolidin-1-yl-propan-1-one (L)-(+)tartrate salt, a pharmaceutical composition comprising said salt, a process for making said salt, and the use of said salt in the treatment of pain.

Abstract: Methods for preparing Ritodrine hydrochloride are provided. Also provided is non-hygroscopic, crystalline, polymorphic Ritodrine hydrochloride of Form I.

Abstract: Methods for preparing Ritodrine hydrochloride are provided. Also provided is non-hygroscopic, crystalline, polymorphic Ritodrine hydrochloride of Form I.

Abstract: A method is described for preparing argatroban monohydrate obtained from (2R,4R)-1-[NG-nitro-N2-(3-methyl-8-quinolinesulphonyl)-L-arginyl]-4-methyl-2-piperidine carboxylic acid by suitably treating crude argatroban. The method either comprises preparation of argatroban monohydrate in a continuous step or an intermediate step of isolating a purified argatroban. Also obtainable from argatroban monohydrate is anhydrous argatroban, shown to have new physico-chemical characteristics. The described argatroban synthesis and purification process hence enables three different forms of argatroban, not previously described, to be obtained, each with distinctive physico-chemical characteristics and in particular enables argatroban monohydrate to be obtained with high yield and with high purity, being therefore a product suitable for use as active principle in proprietary medicines.

Abstract: A method is described for preparing argatroban monohydrate obtained from (2R,4R)-1-[NG-nitro-N2-(3-methyl-8-quinolinesulphonyl)-L-arginyl]-4-methyl-2-piperidine carboxylic acid by suitably treating crude argatroban. The method either comprises preparation of argatroban monohydrate in a continuous step or an intermediate step of isolating a purified argatroban. Also obtainable from argatroban monohydrate is anhydrous argatroban, shown to have new physico-chemical characteristics. The described argatroban synthesis and purification process hence enables three different forms of argatroban, not previously described, to be obtained, each with distinctive physico-chemical characteristics and in particular enables argatroban monohydrate to be obtained with high yield and with high purity, being therefore a product suitable for use as active principle in proprietary medicines.

Abstract: A process for the preparation of ziprasidone and a novel intermediate useful in its preparation. The process comprises the reduction of a compound (III) to give a compound (V) which is then reduced to compound (II). This is reacted with compound (IV) to give the desired compound.

Abstract: The present invention relates to a novel method for manufacture of sertindole comprising manufacturing 5-chloro-1-(4-fluorophenyl)-indole and converting it to sertindole wherein the method for manufacture of 5-chloro-1-(4-fluorophenyl)-indole comprises reacting 5-chloro-indole with a 4-fluorophenylhalide in the presence of a base, a chelating ligand and catalytic amounts or a copper salt comprising copper(I) or copper(II) and an anion which does not interfere in an unfavourable way with the reaction.