426 results about "Mesylate" patented technology

The invention relates to an olefin two-phase hydroformylation method, which consists of three parts: polyether guanidine mesylate ionic liquid (PGMILs) with room temperature solidifiable characteristics, complex catalysts (Rh-TPPTS) formed by RhCl3.3H2O or dicarbonylacetylacetonato rhodium and triphenylphosphine sodium trithionate (TPPTS), and reactants of C6-C14 straight chain 1-olefin, wherein the Rh-TPPTS is dissolved in the PGMILs to form a lower layer catalyst phase, the C6-C14 straight chain 1-olefin or product aldehyde forms an upper layer organic phase, the selectivity of high-carbon aldehyde is 85 to 99 percent, the mol ratio of normal aldehyde to isomerism aldehyde is 2.0 to 2.4, the PGMILs phase containing Rh-TPPTS can be cyclically used for 35 times, the activity and the selectivity are unchanged, the accumulated conversion number (TON) reaches higher than 30000, rhodium flowing to the product phase is 0.04 percent to 0.07 percent, and ultra-long-period catalysis activity and selectivity can be realized.

The invention relates to a method for preparing Decitabine. The particular proposal for solving the technical problem is as follows: 2-deoxidtion-D-ribose, 10 percent of HCL methanol solution, methoxyacetic acetic anhydride, HMDS, acetic anhydride, tri-silicyl tri-fluorine methane sulfonic acid ester, acetic acid amine, etc. are adopted as raw materials to synthesize the Decitabine; the target product of the Decitabine is obtained through the five steps of reactions, namely, methylation, acylation, trimethyl silication, ammoniation and deacylation with a total yield of above 18.4 percent and a product purity of above 99.7 percent.

The invention belongs to the technical field of medicines and discloses cytarabine 5'-O-amino-acid ester, pharmaceutically acceptable salts thereof and a preparation method thereof. The preparation method comprises the following steps of: slowly dropping carbobenzoxy chloride into a solution formed by cytarabine, sodium bicarbonate and N,N-dimethylacetylamide, and obtaining a compound A after reacting at room temperature; using the compound A and N-butyloxy formoxyl-amino acid as raw materials; adding a reagent to the solution to carry out an esterification reaction to obtain the cytarabine 5'-O-amino-acid ester; and then adding acid to obtain a finished product. The pharmaceutically acceptable salts comprise hydrochlorides, sulfates, formates, acetates, mesylates, propionates, butyrates, p-toluene sulphonates, phosphates, bisulfates, maleates, lactates, carbonates, bicarbonates, malonates, and salts formed with acidic amino acids, and the like. The invention can obviously improve the membrane permeability of the cytarabine so as to improve the bioavailability of the cytarabine.

This invention relates to an anti-infective compound, more specifically, 6-fluoro-1-methyl-4-oxo-7-(1-piperazine)-4H-[1, 3] thiazine [3, 2-a] quinoline-3-carboxylic mesylate (compound I), its preparation method and its application. Compound I is prepared by reaction of 6-fluoro-1-methyl-4-oxo-7-(1-piperazine)-4H-[1,3]thiazine[3,2-a]quinoline-3-carboxylic acid and methyl sulfonic acid. Compound I can be used as effective component and mixed with normal pharmaceutical carrier to manufacture anti-infective drug composition, which can be tablets, capsules, granules, injection, eye preparations, ear preparations, gynecological preparations, and external use preparations. Compound I has stable properties, and can be easily dissolved in water, thus can be easily manufactured into various preparations used in clinical treatment. The method has such advantages as simple and reasonable process.

The invention discloses 4-alkyl-2-arylamino-5-(1,2,4-triazole-1-group) thiazole and salts thereof shown in a formula I, wherein R is selected from H, alkyl groups of C1-C2 and straight-chain alkyl groups or branched-chain alkyl groups of C3-C4; X1, X2, X3, X4 and X5 are selected from hydrogen, alkyl groups of C1-C2, hydroxide group, methoxy group, oxyethyl group, trifluoromethyl, fluorine, chlorine, bromine, nitryl, amino group, acetyl amino group, methanesulfamide, ethoxycarbonyl or carboxyl; and the salts of the 4-alkyl-2-arylamino-5-(1,2,4-triazole-1-group) thiazole are selected from hydrochloride, hydrobromide, nitrate, sulfate, phosphate, mesylate, p-toluene sulfonate, tartrate, lactate or malate. The 4-alkyl-2-arylamino-5-(1,2,4-triazole-1-group) thiazole is applied to preparation of medicaments for resisting cervical cancer or lung neoplasms.

The invention belongs to the field of pharmaceutical synthesis, and relates to impurities in a raw medical material production process and preparation methods of the impurities, in particular to preparation methods of process impurities A, B and C of lenvatinib mesylate, namely, 4-[3-chloro-4-(N'-cyclopropylureido) phenoxy]-7-methoxyquinoline-6-carboxamide mesylate), as a drug for treating radioiodine-refractory thyroid cancer and an application of the impurities to quality research of lenvatinib mesylate. With adoption of the methods, the process impurities A, B and C are obtained through chemical synthesis for the first time, and the target compounds shown in the description can be obtained through efficient and rapid separation.

The invention provides a preparation method of trifluoro methanesulfonic anhydride. The method comprises the following steps of: firstly reacting trifluoro methanesulphonyl fluoride with alkali metal hydroxide to prepare trifluoro mesylate, purifying trifluoro mesylate by recrystallization by utilizing an organic solvent, reacting trifluoro methane sulfonyl chloride with trifluoro mesylate to generate a trifluoro methanesulfonic anhydride crude product, and finally purifying trifluoro methanesulfonic anhydride by atmospheric distillation. The preparation method of trifluoro methanesulfonic anhydride can be used for not only effectively simplifying reaction steps so that the operation process is simple and convenient and the operation is safe, but also avoiding byproducts generated in the process of the traditional method for producing trifluoro methanesulfonic anhydride, and effectively reducing the contents of F<-> and SO4<2-> in the product; by utilizing recrystallization, atmospheric distillation and other methods for purification, the product purity is up to 99.5%; and more importantly, the yield of anhydride is greatly increased and raised to 88% from original 60%.

The invention belongs to the technical field of medicines, and particularly relates to a pharmaceutical salt of AZD9291 and a preparation method thereof. The novel pharmaceutical salt of AZD9291 disclosed by the invention is maleate, fumarate, gluconate, malonate, succinate or lactate. AZD9291 reacts with maleic acid, fumaric acid, gluconic acid, malonic acid or succinic acid in a ketone or alcohol solvent, and by crystallization, the pharmaceutical salt is obtained. Compared with AZD9291 mesylate, the pharmaceutical salt of AZD9291 provided by the invention has lower hygroscopicity, overcoming the problem that the conventional AZD9291 mesylate can easily deliquesce, and therefore is more suitable for medicine development.

The invention relates to the technical field of a preparation method of an antithrombotic medicament Prasugrel. The preparation method condenses and synthesizes 2-cyclopropyl-1-(2-fluorophenyl)-2- carbonyl ethyl ester mesylate and 2-methoxyl-4, 5, 6, 7-tetrahydro-thieno (3, 2-c) pyridine to form the Prasugrel. Compared with the prior art, the preparation method provided by the invention has low toxicity in raw materials and reagents used, low requirements in labor protection, low prices of and easy access to raw materials and reagents, less emission of three wastes (waste gas, waste water andwaste residues) and no corrosion to equipment during the production; simultaneously, the preparation method also has tender reaction conditions, simple operation and greater yield compared with the prior art and is applicable to industrial mass production.

The invention relates to a preparation method of fulvestrant. The preparation method comprises a step of implementing reaction on a fulvestrant intermediate body (represented as formula II) and S-(4,4,5,5,5-pentafluoro amyl) isothiourea mesylate to introduce a pentafluoro amyl sulfenyl group, and further comprises a step (ii) of removing a protecting group of hydroxyl and/or a step iii) of oxidizing thioether into sulfoxide according to demand. According to the preparation method disclosed by the invention, raw materials are convenient to prepare and the post-processing is relatively simple, the yield of a target product is increased, the production cost is reduced, and the fulvestrant is applicable to large-scale industrial production.

A process is provided for the preparation of compounds of formula I, useful in the preparation of compounds such as Omeprazole, Lansoprazole and Pantoprazole, wherein R1=H or CH3, R2=H or CH3, R3=Alkoxy (1-4C), OCH2CF3, Cyano, Hydrogen, Halogen, Acetoxy or Aryloxy, any electron withdrawing group or salts (organic or inorganic) of electron donating groups, R=Alkoxy, Hydroxy, Halogen, Activated ester, Tosylate, Mesylate, Thiol or Xanthyl, wherein the process for the preparation of compound of formula I employs a free radical reaction to functionalize the 2-position.

The invention belongs to the technical field of medicines and particularly relates to a ropivacaine mesylate compound. The structural formula of the ropivacaine mesylate compound is shown in the description, and an X-ray powder diffraction spectrogram obtained by measuring the ropivacaine mesylate compound with Cu-K alpha rays is shown in figure 1. The invention also provides a preparation process of the ropivacaine mesylate compound, a pharmaceutical composition containing the ropivacaine mesylate compound and a preparation process of the pharmaceutical composition. Dosage forms of the ropivacaine mesylate pharmaceutical composition are powder injections, small volume injections and large volume injections. The ropivacaine mesylate compound is high in solubility and high in dissolution rate, and the pharmaceutical composition of the ropivacaine mesylate compound is good in dissolubility, easy to dissolve and composite and high in bioavailability.