140947-23-5Relevant articles and documents
Preparation method of ketorolac
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, (2022/04/16)
The present invention relates to the field of medicine, specifically a method of preparation of ketorolac, in the process of preparing ketorolac using alkaline hydrolyzed intermediate A5, borohydride is added, the sample of ketorolac obtained is examined in accordance with the Chinese Pharmacopoeia solution color inspection method, significantly lighter than the sample color obtained by the prior art, the preparation method of ketorolac of the present invention, compared with the prior art in the process of salting with tromethamine, compared with the method of using reducing sulfide in the process of salting with tromethamine, can avoid the risk of incandescent residue unqualified, providing convenience for the staff.
Ketorolac tromethamine intermediate compound VI
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Paragraph 0082-0094, (2021/07/11)
The invention belongs to the technical field of drug synthesis, and particularly relates to a ketorolac tromethamine intermediate compound VI. The synthesis method of the ketorolac tromethamine intermediate compound VI comprises the following steps: adding a compound V into a reaction solvent, slowly adding alkali in batches at controlled temperature, reacting at constant temperature after the addition is finished, cooling after the reaction is finished, dropwise adding a compound IV into the reaction system, performing temperature-controlled reaction after dropwise adding is completed, and adjusting pH after the reaction is completed; evaporating under reduced pressure to remove the solvent, adding an extraction solvent into residues for extraction, collecting an organic layer, filtering and drying to obtain the compound VI. The invention provides a novel method for synthesizing a ketorolac tromethamine intermediate compound by using the intermediate, and the method is simple and convenient to operate; starting raw materials are easy to obtain, highly toxic and highly corrosive substances are not used in the reaction, the reaction steps are few, the operation is simple, and the method is suitable for industrial production; the reaction speed is high, impurities are few, the reaction yield and purity are improved, and the cost is reduced.
Improved preparation method of ketorolac intermediate
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Paragraph 0041-0052, (2021/07/01)
The invention discloses an improved preparation method of a ketorolac intermediate. The intermediate is (5-Benzoyl-1H-pyrrol-2-yl)methanetricarboxylic acid triethyl ester (M-1). The method comprises the following steps: subjecting 2-benzoylpyrrole, methane tricarboxylic acid triethyl ester, manganese acetate dihydrate (trivalent), sodium acetate and acetic anhydride to reacting in an organic solvent; adding an aqueous sodium hydrogen sulfite solution for extraction and liquid separation; and conducting vacuum concentration on an organic phase and pulping the an organic phase with an alcohol solvent. According to the method, post-treatment problems caused by the existence of a large amount of manganese ion compounds and a large amount of solvent acetic acid are effectively solved; meanwhile, the problems of high energy consumption, long period, high cost and the like caused by later concentration are reduced; and the obtained intermediate has the advantages of high purity, high yield and the like and is suitable for industrial production.