Patent classifications
C07F9/025
PROCESSES FOR PURIFYING LIGANDS
Embodiments of the present invention are directed to processes for purifying ligands such as organopolyphosphite ligands. In one embodiment, a process comprises: (a) receiving a solid organopolyphosphite compound that has been recrystallized or triturated at least once, wherein the solid organopolyphosphite compound comprises greater than one weight percent of an oxidized phosphite impurity and wherein the organopolyphosphite compound is substantially free of solvent; (b) slurrying the solid organopolyphosphite compound in a C.sub.2 or higher alcohol at a temperature of at least 60 C. for at least 20 minutes to reduce the oxidized phosphite impurity in the solid phase; and (c) removing liquid comprising dissolved oxidized phosphite impurity from the slurry, wherein the residual oxidized phosphite impurity content of the organopolyphosphite compound following step (c) is 1 weight percent or less.
Phosphoramidate compound and preparation method and crystal thereof
The present disclosure involves a composition enriched in compound 61501b, wherein the compound 61501b has a purity of not less than 90% or more. The composition has a significant advantage in preparing a high-purity compound Sp-1. In addition, the present disclosure also provides a preparation method of the composition enriched in compound 61501b. The method adopts a crystallization technique to perform separation and purification, has a simple and convenient operation and good reproducibility, and therefore the compound 61501b in the prepared composition has high purity and quality. Further, the present disclosure also involves a novel crystal form of compound 61501b.
Phosphorus control for waste streams from glyphosate manufacturing processes
This invention relates to processes for the removal of phosphorous from aqueous waste streams comprising phosphorus-containing compounds produced in the manufacture of glyphosate, in order to meet and typically exceed environmental regulations. More particularly, various embodiments of the present invention relate to the removal of phosphorous-containing compounds utilizing biological treatment system(s), oxidizing agent(s), and/or precipitant(s). The processes of the invention are also applicable to the removal of phosphorous compounds from phosphorous-containing waste streams other than those waste streams resulting from the manufacture of glyphosate.
POLYMORPH OF SODIUM NERIDRONATE AND PREPARATION PROCESS THEREOF
The present invention relates to a novel crystalline hemihydrate polymorph of neridronic acid sodium salt, and a novel process for the preparation thereof comprising the steps of: 1) dissolving solid sodium neridronate in any crystalline form in water, at a temperature in the range from 70 to 90 C., to obtain an aqueous solution of sodium neridronate; 2) adding a solvent selected from the group consisting in ethanol, 1-propanol, and 2-propanol to the aqueous solution obtained from step (1), so that the final water:solvent volume ratio is in the range from 1:0.5 to 1:1, thus obtaining a suspension; 3) placing the suspension obtained from step (2) under mechanical stirring, at a temperature in the range from 60 to 95 C.; 4) recovering the crystalline hemihydrate form F of sodium neridronate formed in the previous step (3). The crystalline hemihydrate form F of sodium neridronate, particularly stable, may be employed in the preparation of solid oral pharmaceutical forms for use in the treatment of musculoskeletal and calcium metabolism disorders.
SOLUTION COMPRISING THE CHLORIDE HYDROCHLORIDE SALT OF 4-(5-(2-(3,5-BIS(TRIFLUOROMETHYL)PHENYL)-N,2-DIMETHYLPROPANAMIDO)-4-(o-TOLYL)PYRIDIN-2-YL)-1-METHYL-1-((PHOSPHONOOXY)METHYL)PIPERAZIN-1-IUM (FOSNETUPITANT) AND PALONOSETRON HYDROCHLORIDE IN COMBINATION WITH DEXAMETHASONE AS A NEUROKININ RECEPTOR MODULATOR
Disclosed are compounds, compositions and methods for the prevention and/or treatment of diseases which are pathophysiologically mediated by the neurokinin (NK.sub.1) receptor. The compounds have the general formula (I):
##STR00001##
Solution comprising the chloride hydrochloride salt of 4-(5-(2-(3,5-bis(trifluoromethyl)phenyl)-N,2-dimethylpropanamido)-4-(o-tolyl)pyridin-2-yl)-1-methyl-1-((phosphonooxy)methyl)piperazin-1-IUM-(fosnetupitant) and palonosetron hydrochloride in combination with dexamethasone as a neurokinin receptor modulator
Disclosed is a solution comprising the chloride hydrochloride salt of 4-(5-(2-(3,5-bis(trifluoromethyl)phenyl)-N,2-dimethylpropanamido)-4-(o-tolyl)pyridin-2-yl)-1-methyl-1-((phosphonooxy)methyl)piperazin-1-ium (fosnetupitant) and palonosetron hydrochloride in combination with dexamethasone and its application in methods for preventing acute and delayed nausea and vomiting in a human patient receiving highly emetogenic cancer chemotherapy.
Process for the synthesis of substituted chloromethyl dialkylphosphates
Disclosed are compounds including phosphate and N-oxide prodrugs of the NK1 antagonist netupitant, useful in the prevention and/or treatment of diseases including emesis induced by chemotherapy. Also disclosed are methods of making a di-tert-butyl (chloromethyl) phosphate useful in the manufacture of such prodrugs by reacting a dialkylphosphate salt with an acid to obtain the corresponding ester of phosphoric acid, reacting the ester with a quaternary ammonium hydroxide base to form a monobasic salt, and reacting the monobasic salt with chloroiodomethane to form the corresponding chloromethyl dialkyl phosphate. ##STR00001##
Phosphoramidate Compound and Preparation Method and Crystal Thereof
The present disclosure involves a composition enriched in compound 61501b, wherein the compound 61501b has a purity of not less than 90% or more. The composition has a significant advantage in preparing a high-purity compound Sp-1. In addition, the present disclosure also provides a preparation method of the composition enriched in compound 61501b. The method adopts a crystallization technique to perform separation and purification, has a simple and convenient operation and good reproducibility, and therefore the compound 61501b in the prepared composition has high purity and quality. Further, the present disclosure also involves a novel crystal form of compound 61501b.
SUBSTITUTED 4-PHENYL-PYRIDINES
Disclosed are compounds, compositions and methods for the prevention and/or treatment of diseases which are pathophysiologically mediated by the neurokinin (NK.sub.1) receptor. The compounds have the general formula (I):
##STR00001##
Substituted piperaziniums for the treatment of emesis
Disclosed are compounds, compositions and methods for the prevention and/or treatment of diseases which are pathophysiologically mediated by the neurokinin (NK.sub.1) receptor. The compounds have the general formula (I): ##STR00001##