1408238-40-3Relevant articles and documents
Preparation method of anticoagulant drug dabigatran etexilate and analogues thereof
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Paragraph 0056-0059, (2020/05/01)
The invention discloses a preparation method of an anticoagulant drug dabigatran etexilate and analogues thereof. The preparation method comprises the following steps: 3-[(3-amino-4-methylaminobenzoyl)pyridin-2-ylamino]propionic acid ethyl ester (DGM1) and isopropyl 2-(4-cyanophenylamino)acetate (DGM2) which are taken as reaction initial raw materials undergo a docking reaction under the action ofan alkali reagent and a condensing agent to prepare an intermediate DG1; the intermediate DG1 reacts in an alcohol solvent to produce imino ester, and acid catalysis and ammonia reaction are carriedout to prepare a formamidine compound; an intermediate DG2 reacts with n-hexyl chloroformate under the action of the alkali reagent to remove one molecule of water and form an amido bond in order to obtain dabigatran etexilate; and the dabigatran etexilate analogues DG-D1 to DG-D4 are prepared from the dabigatran etexilate and its intermediate DG2. The preparation method of the dabigatran etexilate and analogues thereof has the advantages of short and feasible synthesis route, simplicity in operation, high product yield is high, and suitableness for large-scale industrial production.
A preparation darbey adds the group ester amide the method of impurity (by machine translation)
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Paragraph 0030; 0031; 0034; 0035, (2016/11/24)
The present invention relates to the field of organic synthesis technology, in particular to a kind of preparation darbey adds the group ester amidation method of the impurity, the method to 4-aminobenzoic amidine-Carbamic N-own ester as the raw material, prepared by the hydrolysis reaction of hydrolysis product, then the hydrolysis product and the 3 - [(3-amino-4-methyl-aminobenzoyl) pyridin-2-yl-amino] propionic acid ethyl ester under the action of catalyst and undergo condensation, get darbey adds the group ester amide impurity, the method can be obtained through the two step process of the finished product darbey adds the group ester amide impurity, the method is simple, easy to operate, and does not need the chromatographic separation is a compound of high purity can be obtained, to darbey adds the group ester control the quality of the drug impurities provide a high-purity of the substance. (by machine translation)