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Authors
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Jopp, S. ; Molenda, R. ; Seiler, E.R.D. ; Maitz, M.F. ; Villinger, A. ; Ehlers, P. ; Langer, P.
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Title
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Total synthesis of dabigatran revisited; Synthesis of amidine-tosylated dabigatran
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Date
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19.12.2019
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Number
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58023
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Abstract
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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. In this context, it was found that, in our hands, a published synthesis did not work as reported. Part of the synthetic strategy presented herein is an amidine–selective tosylation of 4–aminobenzamidine. Furthermore, two new dabigatran derivatives exhibit thrombin inhibition activity.
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Publisher
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Chemistry Select
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Wikidata
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Citation
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Chemistry Select 4 (2019) 13802-13805
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DOI
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https://doi.org/10.1002/SLCT.201903881
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Tags
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