The total synthesis of a new dabigatran derivative featuring a tosyl protecting group at the amidine group of dabigatran was explored. During the course of this work, different new synthetic pathways towards dabigatran intermediates are investigated and known concepts revisited.
The invention discloses dabigatran etexilate, an intermediate thereof with a formula (5), and a synthesis method of a derivative thereof.
The present invention describes an improved process for the preparation of Dabigatran Etexilate (Formula-I), a pharmaceutically acceptable salt for the treatment of thromboses, cardiovascular.
Synthetic impurities that are present in dabigatran etexilate mesylate were studied, and possible pathways by which these impurities are formed during the manufacturing process were examined. The impurities were monitored by high-performance liquid chromatography, and their structures were determined by mass spectrometry and 1 H and 13 C NMR.
One of the advanced intermediates as per reported process for the preparation of Dabigatran Etexilate is compound of formula (VI). The compound of formula (VI) is prepared by a reaction of compound of formula (IV) and compound of formula (V) with reagent as shown in Scheme 1.
The present invention relates to new processes for the preparation of synthesis intermediate products useful in the preparation of Dabigatran Etexilate on an industrial scale. The invention also.
An improved process for the preparation of dabigatran etexilate mesylate, wherein the process is substantially free to eliminates the potential impurities. The impurities are formed due to presence of contaminated starting ingredients that is present in commercially available n-hexyl chloro formate.
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. (WO2015124764) SYNTHESIS PROCESS OF DABIGATRAN ETEXILATE MESYLATE, INTERMEDIATES OF THE PROCESS AND NOVEL POLYMORPH OF DABIGATRAN ETEXILATE click herefor patent.
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Objective: To study and improve the synthesis proccess of dabigatran etexilate mesylate. Methods: The intermediate ethyl 3-((3-amino-4-(methylamino)benzoyl) (pyridin-2-yl) amino)-propanoate (5.
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PROCESS FOR THE MANUFACTURE OF AN INTERMEDIATE IN THE SYNTHESIS OF DABIGATRAN (PAT - WO2009153214) HEDDESHEIMER INGO, SCHOLZ ULRICH. BOEHRINGER INGELHEIM INT. Patent: Publ.of the Int.Appl. with Int.search report - World Intellectual Property Organization.
PROCESS FOR THE MANUFACTURE OF AN INTERMEDIATE IN THE SYNTHESIS OF DABIGATRAN (PAT - EP2300431) HEDDESHEIMER INGO, SCHOLZ ULRICH BOEHRINGER INGELHEIM INT. Patent: Publ. of Application with search report - European Patent Office. Application.
PROCESS FOR THE MANUFACTURE OF AN INTERMEDIATE IN THE SYNTHESIS OF DABIGATRAN (PAT - US2011295018) HEDDESHEIMER INGO, SCHOLZ ULRICH. BOEHRINGER INGELHEIM INT. Patent: Patent Appl. Publ. within the TVPP - United States. Application: US20090997349 on 2009-06.