A kind of preparation method of oteracil potassium
A technology of oteracil potassium and potassium iodide, which is applied in the field of preparation of oteracil potassium, can solve the problems of low operation safety, long reaction time, and many impurities generated, and achieves safe and convenient operation, short reaction time, high purity  high effect
Active Publication Date: 2022-05-31
LUNAN PHARMA GROUP CORPORATION
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[0015] Aiming at the problems of low conversion rate, long reaction time, many impurities and low operation safety existing in the current preparation process, the present invention aims to provide a method with simple operation, mild reaction conditions, high product yield and high purity.  A preparation method suitable for industrialized production of oteracil potassium with less pollution
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The invention provides a preparation method of oteracil potassium.  The method comprises the steps of: dissolving allantoin, alkali and potassium iodide in purified water at room temperature, adding N-halogenated amides in batches after the reaction solution is cooled, and heating up the reaction after the addition is completed. After the reaction is detected, the reaction solution is  Lower the temperature, adjust the pH with acid, stir and grow the crystal, and filter with suction. The filter cake is washed with cold purified water until it is colorless, then rinsed with cold anhydrous alcohol solvent, and dried in vacuum to obtain oteracil potassium.  Compared with the prior art, the whole process has simple and easy raw materials, easy operation, mild reaction conditions, stable quality, high yield, no pollution to the environment, and is suitable for industrialized production.
Description
A kind of preparation method of oteracil potassium   technical field   The invention belongs to the technical field of medicinal chemistry, be specifically related to a kind of preparation method of oteracil potassium.   Background technique   Compound that the present invention relates to is oteracil potassium (Potassium oxonate), has another name called potassium oxonate, chemical   Name: 1,4,5,6-tetrahydro-4,6-dioxy-1,3,5-triazine-2-potassium carboxylate, chemical structural formula is as follows:   [0003]   Oteracil potassium is one of three kinds of active medicines in oral anticancer compound medicine Sigirone Capsules, Seggio Capsules   It is an oral anticancer agent of fluorouracil derivatives, mainly composed of tegafur and two biochemical regulators, gimeracil and oteracil.   It is composed of western potassium, among which tegafur has excellent oral bioavailability and can be converted into 5-fluorouracil in the body; gimeracil   It can inhibit the degradation of 5-fluoro...
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IPC IPC(8): C07D251/20
CPCC07D251/20
 Inventor 王洪刚朱安国
 Owner LUNAN PHARMA GROUP CORPORATION
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