212322-56-0Relevant articles and documents
Synthesis, Crystal Structure, and Anti-Gastric Cancer Activity of Ethyl 3-(3-Amino-4-(Methylamino)-N-(Pyridin-2-Yl) Benzamido)Propanoate
Liu,Peng,Yue,Li,Zhang
, p. 2009 - 2014 (2019)
A new heterocyclic compound ethyl 3-(3-amino-4-(methylamino)-N-(pyridin-2-yl)benzamido)propanoate (1), designed using 4-(methylamino)-3-nitrobenzoic acid (2) as a starting material is successfully obtained via a multiple synthesis route and finally characterized by IR, 1H NMR, and single crystal X-ray crystallography. In addition, the in vitro anti-cancer activity of newly synthesized complex 1 is emulated against three human gastric cancer cell lines SGC-790, MKN-4, and MKN45.
Dabigatran etexilate key intermediate preparation method
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Paragraph 0028; 0029; 0030; 0031; 0032; 0033, (2019/10/01)
The invention relates to the field of pharmaceutical intermediates, particularly to an industrial preparation method of a dabigatran etexilate key intermediate. According to the preparation method, astarting raw material is subjected to nitro reduction, amide condensation and cyclization reaction to obtain a key intermediate 3-{2-[(4-cyanophenylamino)methyl]-1-methyl-N-(pyridine-2-yl)-1H-benzo[d]imidazole-5-amido}ethyl propionate. According to the present invention, the preparation method can reduce the production cost, make the production process safe, and improve the yield, and is suitablefor industrial large-scale production.
A process for preparing darbey adds the group ester method
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Paragraph 0028; 0033; 0035; 0040; 0042; 0047, (2017/08/25)
The invention discloses a dabigatran etexilate preparation method. The method comprises the following steps: preparing an intermediate 1, preparing an intermediate 2, preparing an intermediate 3, preparing an intermediate 4, preparing an intermediate 5, preparing an intermediate 6, and preparing dabigatran etexilate. The preparation method has the advantages of cheap and easily available raw materials, easy operation, easy control, high reaction yield, high product purity, and suitableness for the large-scale industrial production of dabigatran etexilate.
Synthesis method of benzimidazole compound K
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Paragraph 0043; 0044, (2017/03/08)
The invention provides a synthesis method of a benzimidazole compound K. The method includes the steps of: 1) producing a compound 2 from a compound 1 under the action of a reducing agent; 2) subjecting the compound 2 and an acylation reagent to cyclization to generate a compound 3; 3) producing a compound 5 from nitrobenzamide 4 and hexyl chloroformate in the existence of strong base; 4) conducting catalytic hydrogenation on the compound 5 under certain hydrogen pressure to reduce nitro into amino so as to generate a compound 6; and 5) producing the compound 3 and the compound 6 into the benzimidazole compound K under certain temperature in the existence of sodium iodide and weak base, with the synthetic route shown as the specification. The method provided by the invention adopts cheap and easily available raw materials to achieve oriented synthesis of the benzimidazole compound K by 5-step reaction, the obtaine product has no need for purification, the aftertreatment of each step is simple, and the product is convenient to obtain. Therefore, the method is suitable for large-scale synthesis, and provides standard substances for quality research.
Multi-substituted 4-methyl ester derivative of amino benzonitrile trunk and its preparation and use
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Paragraph 0096; 0114-0116, (2018/01/19)
The invention provides new ester derivatives with a general formula (I) shown in the specification of multi-substituted 4-methylamino-benzamidine or pharmaceutically acceptable salts, wherein A1, A2, A3 and A4 in the formula are as defined in the specification. The compounds have an anticoagulant effect and can be used for preparing medicaments for preventing and treating thromboembolic diseases.
Preparation technique of dabigatran methanesulfonate
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Paragraph 0053; 0054, (2016/10/10)
The invention discloses a preparation technique of dabigatran methanesulfonate. The technique comprises the following steps: 1) by using a compound I and glycine as raw materials, carrying out condensation and salification to obtain a compound II; 2) by using p-halobenzonitrile (III) as a raw material, synthesizing p-halobenzamidine (IV) under the actions of a catalyst and an aminating agent, and carrying out condensation on the p-halobenzamidine (IV) and n-hexyl chloroacetate to obtain a compound V; and 3) carrying out condensation and salification on the compound V and the compound II to obtain the dabigatran methanesulfonate. The synthesis method has the advantages of mild reaction conditions for each step and high selectivity, and is simple to operate. The dabigatran methanesulfonate has high yield and purity. The technique has the advantages of less discharge of three wastes and environment friendliness, does not need column chromatography purification, and is suitable for industrial production.
PROCESS FOR THE PREPARATION OF DABIGATRAN ETEXILATE MESYLATE AND POLYMORPHS OF INTERMEDIATES THEREOF
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Paragraph 0119-0120, (2015/02/18)
The present invention provides crystalline form of intermediates of Formula 2A, The present invention also provides process for the preparation of dabigatran etexilate mesylate; polymorph of intermediates thereof; particularly processes for the preparation of crystalline form of intermediates. The present invention also relates to the use of crystalline intermediates for the preparation of dabigatran etexilate mesylate.
Process For The Preparation Of Benzimidazole Derivatives And Salts Thereof
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Paragraph 0226, (2015/03/31)
Provided are novel salts of benzimidazole derivatives, preferably salts of benzimidazole derivatives which are useful intermediates in the synthesis of pure 1-methyl-2-[N-[4-(N-n-hexyloxycarbonylamidino)phenyl]aminomethyl]benzimidazol-5-yl-carboxylicacid-N-(2-pyridyl)-N-(2-ethoxycarbonylethyl)amide and its salts.
A PROCESS FOR PREPARATION OF DABIGATRAN ETEXILATE MESYLATE AND INTERMEDIATES THEREOF
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Page/Page column 43; 44, (2015/09/28)
The present invention relates to an improved process for the preparation of Dabigatran etexilate and its acid addition salts thereof, wherein the said process substantially eliminates the potential impurities. The present invention also relates to an intermediate of Dabigatran etexilate and process for preparation thereof.
SYNTHESIS PROCESS OF DABIGATRAN ETEXILATE MESYLATE, INTERMEDIATES OF THE PROCESS AND NOVEL POLYMORPH OF DABIGATRAN ETEXILATE
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Page/Page column 13, (2015/09/23)
12956PTWO_eng 23 "SYNTHESIS PROCESS OF DABIGATRAN ETEXILATE MESYLATE, INTERMEDIATES OF THE PROCESS AND NOVEL POLYMORPH OF DABIGATRAN ETEXILATE" Abstract A novel process is described for the production of Dabigatran etexilate mesylate, a 5 compound having the following structural formula: and two novel intermediates of said process.
