330942-01-3Relevant articles and documents
A facile method for the synthesis of Betrixaban
Li, Jianye,Chen, Ligong,Yan, Xilong,Li, Yang,Wei, Daiyan,Wang, Donghua
, p. 524 - 526 (2015)
A facile method for the synthesis of N-(5-chloropyridin-2-yl)-2-(4-(N,N-dimethylcarbamimidoyl)benzamido)-5-methoxybenzamide (Betrixaban) from 5-methoxy-2-nitrobenzoic acid is achieved by reduction, acylation, chlorination, acylation and the formation of the amidine. A dechlorinated impurity is avoided in this method. Using tetrahydrofuran as the solvent in the four steps makes its recovery easier. The total yield of the target compound is about 40% and this method is suitable for large-scale production.
Improved preparation method of beta-caraban
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, (2019/08/29)
The invention relates to the fields of organic chemistry and pharmacy, and particularly relates to an improved method for preparing betrixaban. Compared with the prior art, the method has the advantages that the defects of use of high-corrosion hydrogen chloride gas, heavy burden for 'three wastes' treatment, difficult refining and purification of products and the like can be overcome. The method is characterized in that a metal organic compound RMR' (M is selected from Mg and Zn, R is selected from Cl, Br, I, alkyl or aryl, and R' is selected from akly or aryl) is used for reacting with dimethylamine or salt thereof in an aprotic solvent; then the obtained reacting liquid reacts with the compound or salt thereof in a formula II to prepare betrixaban. The improved novel method has the advantages of use of easily available raw materials, mild reaction condition, convenience in operation, excellent product quality and low cost and is suitable for industrial large-scale production.
Preparation method of betrixaban intermediate and betrixaban and product thereof
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Paragraph 0068; 0069, (2018/10/11)
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.