- Preparation method of betrixaban intermediate and betrixaban and product thereof
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The invention relates to a preparation method of a betrixaban intermediate or salt thereof. The method includes: under the action of a catalyst, adding an amide coupling reagent dropwise into a compound shown as formula SM-III and a compound shown as formula SM-I or salts thereof for condensation reaction in an organic solvent to form a compound shown as formula III or a salt thereof, and furtherpreparing the betrixaban intermediate or the salt thereof into betrixaban or a salt thereof. The betrixaban or the hydrochloride thereof prepared by the method provided by the invention basically doesnot contain dechlorinated impurity V or demethylated impurity VI, and has high purity. The method improves the product yield, reduces the use of high corrosive raw materials, is low in cost, and is suitable for industrial production.
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Paragraph 0070; 0071
(2018/10/11)
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- Preparation method of betrixaban
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The invention provides a method for preparing betrixaban. The method comprises the following steps: performing the nucleophilic addition elimination on 5-methoxyisatoic anhydride used as a raw material and 2-amino-5-chloropyridine under the condition of potassium tert-butoxide to obtain N-(5-chloro-2-pyridyl)-5-methoxyl-2-aminobenzamide, allowing a compound 4 to react with cyanobenzoyl chloride to obtain N-(5-chloro-2-pyridyl)-2-[(4-cyano benzoyl) amino]-5-methoxyl benzamide hydrochloride, and finally performing the nucleophilic addition with dimethylamine to obtain a target product betrixaban, wherein the total yield is 57.8 percent. By adopting the preparation method, the raw materials are low in price and easy to get, the reaction conditions are moderate, the reaction controllability is high, and the industrialized application prospect is good.
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Paragraph 0012; 0028; 0029; 0065; 0067; 0068
(2016/10/10)
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- METHODS OF SYNTHESIZING PHARMACEUTICAL SALTS OF A FACTOR XA INHIBITOR
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Novel methods of preparing a compound of Formula I which is an inhibitor of Factor Xa and its maleate salt, are described herein.
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Page/Page column 34-35
(2008/12/05)
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- Unit dose formulations and methods of treating thrombosis with an oral factor Xa inhibitor
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Unit doses of factor Xa inhibitor compounds and methods of using these compounds for inhibiting blood coagulation in a human patient are taught herein. The unit dose of the factor Xa inhibitor compounds disclosed herein required to inhibit coagulation in a primate is lower than the unit dose required to obtain similar levels of coagulation inhibition in other animal models, such as rodents. Also taught are in vitro assays useful in predicting in vivo antithrombotic activity in humans.
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Page/Page column 25
(2008/12/06)
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- Novel pharmaceutical salts and polymorphs of a factor Xa inhibitor
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The present invention provides for salts comprising a compound of Formula I and an acid that has activity against mammalian factor Xa. The present invention is also directed to methods of making the compound of Formula I.
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Page/Page column 11
(2008/06/13)
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