Patent classifications
C07C51/412
METHODS OF SYNTHESIZING A PROSTACYCLIN ANALOG
The present invention provides processes for preparing a prostacyclin analogue of Formula (I) or a pharmaceutically acceptable salt thereof, wherein R.sup.10 is a linear or branched C.sub.1-6 alkyl. The processes of the present invention comprise steps that generate improved yields and fewer byproducts than traditional methods. The processes of the present invention employ reagents (e.g., the oxidizing reagent) that are less toxic that those used in the traditional methods (e.g., oxalyl chloride). Many of the processes of the present invention generate intermediates with improved e.e. and chemical purity; thereby eliminating the need of additional chromatography steps. And, the processes of the present invention are scalable to generate commercial quantities of the final compound.
FLUID MIXING STRUCTURE, CONTINUOUS REACTION UNIT, CONTINUOUS REACTION REACTOR AND METHOD OF USING THE SAME
A fluid mixing structure (10) for mixing at least two fluidic components has a flow inlet port and a flow outlet port and comprises a contraction zone (12), an expansion zone (14), and a retention zone (16), arranged in this order in an inflow direction (IFD) of a fluid flow to flow through said fluid mixing structure (10) and being composed of said at least two fluidic components, and a flow splitter (32) arranged In a space (30) formed by said expansion zone (14) and said retention zone (16) to split said fluid flow in a first sub fluid flow and a second sub fluid flow flowing in a first flow path and a second flow path, respectively, formed in the fluid mixing structure, and to mix said first and second sub fluid flows within said space (30) to generate and discharge a homogenized fluid flow, wherein said flow splitter (32) is arranged and configured to let any flow element of each of said first and second sub fluid flows prior to their mixing have a non-zero average flow component in said inflow direction (IFD).
PROCESS FOR LARGE SCALE PRODUCTION OF 1-ISOPROPYL-3--1H-INDAZOLE OXALATE
The present invention relates to a process suitable for adoption to large scale manufacture of 1-isopropyl-3-{5-[1-(3-methoxypropyl)piperidin-4-yl]-[1,3,4]oxadiazol-2-yl}-1H-indazole oxalate of formula (I), which is a selective 5-HT.sub.4 receptor ligand intended for the symptomatic treatment of Alzheimer's disease and other disorders of memory and cognition like Attention deficient hyperactivity, Parkinson's and Schizophrenia.
PROCESS FOR LARGE SCALE PRODUCTION OF 1-ISOPROPYL-3--1H-INDAZOLE OXALATE
The present invention relates to a process suitable for adoption to large scale manufacture of 1-isopropyl-3-{5-[1-(3-methoxypropyl)piperidin-4-yl]-[1,3,4]oxadiazol-2-yl}-1H-indazole oxalate of formula (I), which is a selective 5-HT.sub.4 receptor ligand intended for the symptomatic treatment of Alzheimer's disease and other disorders of memory and cognition like Attention deficient hyperactivity, Parkinson's and Schizophrenia.
METAL SALT OF AN ALICYCLIC DICARBOXYLIC ACID HAVING EXCELLENT DISPERSIBILITY IN POLYOLEFIN RESIN, PRODUCTION METHOD FOR SAID METAL SALT OF AN ALICYCLIC DICARBOXYLIC ACID, CRYSTAL NUCLEATING AGENT FOR POLYOLEFIN RESIN CONTAINING SAID METAL SALT OF AN ALICYCLIC DICARBOXYLIC ACID, CRYSTAL NUCLEATING AGENT COMPOSITION CONTAINING SAID CRYSTAL NUCLEATING AGENT, POLYOLEFIN RESIN COMPOSITION, AND POLYOLEFIN RESIN MOLDED ARTICLE
Provided is a metal salt of an alicyclic dicarboxylic acid with excellent dispersibility in polyolefin resins, and excellent crystallinity improving effect that is essential as a crystal nucleating agent for polyolefin resins, regardless of processing conditions. A method is also provided for producing the metal salt of an alicyclic dicarboxylic acid; a crystal nucleating agent containing the metal salt of an alicyclic dicarboxylic acid; a crystal nucleating agent composition for polyolefin resins containing the crystal nucleating agent and a fatty acid metal salt; a polyolefin resin composition containing the crystal nucleating agent; and a polyolefin resin molded article obtained using the polyolefin resin composition. Provided is a metal salt of an alicyclic dicarboxylic acid in which the alicyclic dicarboxylic acid is an alkyl substituent-containing cyclohexane-1,2-dicarboxylic acid, and the metal salt is a calcium salt, a hydroxyaluminum salt, a disodium salt, or a dilithium salt.
METAL SALT OF AN ALICYCLIC DICARBOXYLIC ACID HAVING EXCELLENT DISPERSIBILITY IN POLYOLEFIN RESIN, PRODUCTION METHOD FOR SAID METAL SALT OF AN ALICYCLIC DICARBOXYLIC ACID, CRYSTAL NUCLEATING AGENT FOR POLYOLEFIN RESIN CONTAINING SAID METAL SALT OF AN ALICYCLIC DICARBOXYLIC ACID, CRYSTAL NUCLEATING AGENT COMPOSITION CONTAINING SAID CRYSTAL NUCLEATING AGENT, POLYOLEFIN RESIN COMPOSITION, AND POLYOLEFIN RESIN MOLDED ARTICLE
Provided is a metal salt of an alicyclic dicarboxylic acid with excellent dispersibility in polyolefin resins, and excellent crystallinity improving effect that is essential as a crystal nucleating agent for polyolefin resins, regardless of processing conditions. A method is also provided for producing the metal salt of an alicyclic dicarboxylic acid; a crystal nucleating agent containing the metal salt of an alicyclic dicarboxylic acid; a crystal nucleating agent composition for polyolefin resins containing the crystal nucleating agent and a fatty acid metal salt; a polyolefin resin composition containing the crystal nucleating agent; and a polyolefin resin molded article obtained using the polyolefin resin composition. Provided is a metal salt of an alicyclic dicarboxylic acid in which the alicyclic dicarboxylic acid is an alkyl substituent-containing cyclohexane-1,2-dicarboxylic acid, and the metal salt is a calcium salt, a hydroxyaluminum salt, a disodium salt, or a dilithium salt.
IMPROVED PROCESS FOR THE PREPARATION OF [[2(S)-[[4(R)-(3-HYDROXYPHENYL)-3(R),4-DIMETHYL-1-PIPERIDINYL]METHYL]-1-OXO-3-PHENYLPROPYL]AMINO]ACETIC ACID DIHYDRATE
The present invention relates to an improved process for the preparation of [[2(S)-[[4(R)-(3-hydroxyphenyl)-3(R),4-dimethyl-1-piperidinyl]methyl]-1-oxo-3-phenylpropyl]amino]acetic acid dihydrate, represented by the following structural formula (I).
IMPROVED PROCESS FOR THE PREPARATION OF [[2(S)-[[4(R)-(3-HYDROXYPHENYL)-3(R),4-DIMETHYL-1-PIPERIDINYL]METHYL]-1-OXO-3-PHENYLPROPYL]AMINO]ACETIC ACID DIHYDRATE
The present invention relates to an improved process for the preparation of [[2(S)-[[4(R)-(3-hydroxyphenyl)-3(R),4-dimethyl-1-piperidinyl]methyl]-1-oxo-3-phenylpropyl]amino]acetic acid dihydrate, represented by the following structural formula (I).
Solid Forms of Nilotinib Hydrochloride
A solid form of Nilotinib hydrochloride, which exists as a co-crystal of nilotinib hydrochloride and levulinic acid having a molar ratio of nilotinib hydrochloride to levulinic acid of 1:2, and a process for the preparation of the co-crystal.
Solid Forms of Nilotinib Hydrochloride
A solid form of Nilotinib hydrochloride, which exists as a co-crystal of nilotinib hydrochloride and levulinic acid having a molar ratio of nilotinib hydrochloride to levulinic acid of 1:2, and a process for the preparation of the co-crystal.