Abstract: The present invention relates to a method for purifying key intermediates of Citalopram, i.e. 4-[4-(dimethylamino)-1-(4-fluorophenyl)-1-hydroxybutyl]-3-hydroxymethylbenzonitrile and a salt thereof. The method comprises dissolving crude 4-[4-(dimethylamino)-1-(4-fluorophenyl)-1-hydroxybutyl]-3-hydroxymethylbenzonitrile (compound of formula I containing formaldehyde impurity) with an organic solvent, adding a washing solution, controlling the temperature, stirring, leaving to stand for layering, and removing the aqueous layer, so as to obtain a purified organic solution of 4-[4-(dimethylamino)-1-(4-fluorophenyl)-1-hydroxybutyl]-3-hydroxymethylbenzonitrile. The method provided by the present invention can effectively remove aldehyde group-containing impurities in the intermediate. The method of the present invention has the advantages of simple operation, cheap raw materials and mild conditions, and is suitable for large-scale industrial production.

Abstract: The present invention relates to a method for preparing pregabalin by a biological enzyme method. In particular, the method comprises producing pregabalin B and an R-configuration compound C by using a compound A as a raw material under the action of a biological enzyme; performing configuration inversion of the separated and recovered R-configuration compound C under the action of an isomerase to produce an S-configuration compound D; and producing pregabalin B from the compound D under the action of a biological enzyme.

Abstract: A method for preparing voriconazole L-camphorsulphonate and voriconazole. The method for preparing voriconazole L-camphorsulphonate comprises: method 1: dissolving (2R,3S)/(2S,3R) isomer mixture and L-camphor sulphonic acid in water and acetone, and performing crystallisation filtration to obtain voriconazole L-camphorsulphonate; method 2: (a) dissolving a mixture of isomer mixture and L-camphor sulphonic acid in a first solvent and then performing crystallisation filtration; or (a?) dissolving L-camphorsulphonate of the isomer mixture in a first solvent and then performing crystallisation filtration; (b) concentrating the filtrate obtained in step (a) or (a?) into a solid; and (c) dissolving the solid obtained in step (b) in a second solvent and performing crystallisation filtration to obtain voriconazole L-camphorsulphonate. Adjusting the resolution solvent effectively reduces production costs and facilitates recycling of the resolution solvent.

Abstract: The present application relates to a method for citalopram intermediate citalopram diol. The method comprises: first mixing two Grignard reagents required for a reaction; then mixing the mixed Grignard reagents with a raw material 5-cyanophthalide in a temperature-controllable micromixer to obtain a reaction solution; then subjecting the reaction solution to the reaction by means of a reactor to obtain a citalopram diol reaction solution; and then performing operations such as quenching, concentration, extraction, acidification, and crystallization to obtain a qualified product. The citalopram diol provided in the present invention has good selectivity, high yield, high safety, safety and reliability, and little sewage discharge, and is suitable for industrial production.

Abstract: A powder injection of a donepezil semi palmoxiric acid salt, a composition containing the same and a preparation method therefor. The powder injection contains donepezil semi palmoxiric acid salt crystals having an average particle size of 2-52 ?m.

Abstract: Disclosed is N-formyl vortioxetine, and also disclosed is a method for preparing the N-formyl vortioxetine and a stable solid preparation of vortioxetine.

Abstract: Disclosed is a detection method for N-nitrosodimethylamine (NDMA) impurities, comprising: (1) obtaining a test solution containing a sample to be tested; and (2) detecting the test solution by means of gas chromatography-mass spectrometry to determine the content of an N-nitrosodimethylamine impurity in the sample. The method provided in the present invention has a good separating effect, a wide linear range, a high sensitivity and a good method durability, and can detect the content of N-nitrosodimethylamine (NDMA) in the sample rapidly and effectively.

Abstract: A preparing method for high-purity levetiracetam, comprising: adjusting the pH of an extracted aqueous layer obtained by dissociating (S)-?-ethyl-2-oxo-1-pyrrolidineacetic acid (R)-methylbenzylamine salt to 5-9; removing water; adding an organic solvent to form a solution and then performing an esterification reaction with ethyl chloroformate or methylchlorofonmate; and carrying out an ammonolysis reaction to obtain the levetiracetam. The method simplifies production process, increases yield, reduces or even avoids the use of triethylamine in the esterification process, and reduces the emission of a great amount of three wastes.

Abstract: A method for synthesizing valsartan, comprising the steps of: synthesizing a valsartan methyl ester intermediate to obtain a reaction mixture of the valsartan methyl ester intermediate; diluting the reaction mixture by salt water or water, and then using a first extraction solvent to extract the valsartan methyl ester intermediate; adding alkali to an organic layer containing the valsartan methyl ester intermediate for hydrolyzing, removing the organic layer, regulating pH of a water layer to be acidic by using acid, using the first extraction solvent to extract, concentrating a part of solvent, or distilling the solvent to dryness, and then adding a new solvent; finally, crystallizing, filtering, and drying to obtain the valsartan.

Abstract: The present application relates to a synthesis method for cariprazine, comprising performing an acylation reaction between a compound represented by formula (I) and dimethylcarbamoyl chloride in a reaction solvent in the presence of an aqueous solution of an inorganic base, so as to obtain the cariprazine compound represented by formula (II). The synthesis method overcomes defects in the prior art such as a long reaction time, large size impurities and the difficulty of purification, and provides a new method suitable for commercial production wherein the reaction is fast, impurity sizes are small, the product is easily purified, the purity of the product can reach 99.0% or more, and the yield is high.

Abstract: The present invention relates to a method for preparing an intermediate (Formula IV) of sodium elagolix. The intermediate is prepared by the following route. The method has advantages of simple and safe operation, high yield, less environmental pollution, good economic effect and suitability for industrial production, wherein R represents C1-C4 substituted or unsubstituted benzyl or allyl.

Abstract: Related are a JAK kinase inhibitor, a preparation method for same, and applications thereof in the field of medicine, related to the field of medicinal chemistry. Provided is a novel small molecule JAK inhibitor, which has the structure as represented by formula (II). The compound provides improved efficacy and safeness in preventing or treating a JAK-related indication.

Abstract: A powder injection of a donepezil semi palmoxiric acid salt, a composition containing the same and a preparation method therefor. The powder injection contains donepezil semi palmoxiric acid salt crystals having an average particle size of 2-52 ?m.

Abstract: A powder injection of a donepezil semi palmoxiric acid salt, a composition containing the same and a preparation method therefor. The powder injection contains donepezil semi palmoxiric acid salt crystals, and the average grain size of the crystals ranges from 0.5 ?m to 100 ?m.

Abstract: The present invention relates to a new preparation method for escitalopram pamoate ((S)-(+)-1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-5-cyanoisob enzofuran pamoate), wherein the method is environmentally friendly and pollution-free, and the escitalopram pamoate prepared by means of the method has a high purity and a good repeatability.

Abstract: The present application relates to a synthesis method for cariprazine, comprising performing an acylation reaction between a compound represented by formula (I) and dimethylcarbamoyl chloride in a reaction solvent in the presence of an aqueous solution of an inorganic base, so as to obtain the cariprazine compound represented by formula (II). The synthesis method overcomes defects in the prior art such as a long reaction time, large size impurities and the difficulty of purification, and provides a new method suitable for commercial production wherein the reaction is fast, impurity sizes are small, the product is easily purified, the purity of the product can reach 99.0% or more, and the yield is high.

Abstract: Provided herein is a method for preparing an Escitalopram bis-hydroxynaphthoate ((S)-(+)-1-(3+(dimethylamino)propyl)-1-(4-fluorophenyl)-1,3-dihydro-5-cyanisobenzofuranone) crystal form A. Said method is ecofriendly and non pollutive, and the obtained Escitalopram bis-hydroxynaphthoate crystal form A is highly pure and easy to reproduce.

Abstract: Provided are a fosaprepitant phosphate intermediate (IV) preparation method, a fosaprepitant phosphate intermediate (IV-A) and a method of (AA) for preparing fosaprepitant dimeglumine by using the intermediate (IV-A). IV: R1 and R2 are independently selected from C1-C7 alkyl groups or benzyl groups; IV-A: R1 and R2 are independently selected from C1-C7 alkyl groups, and R1 and R2 are not both benzyl groups.

Abstract: Disclosed are a class of ?-opioid receptor agonists and a preparation method therefor and the use thereof in the field of medicine, belonging to the field of medicinal chemistry. The ?-opioid receptor agonists significantly increase the selectivity for a G protein signaling pathway, and not only can exhibit excellent pharmacodynamic effects, but also significantly improve safety.

Abstract: Disclosed is a new method for preparing a donepezil pamoate (1-benzyl-4-[(5,6-dimethoxyindan-2-one)methyl]piperidine pamoate). The donepezil pamoate prepared by using the method has a high purity and a good flowability.