Authors Jopp, S. ; Molenda, R. ; Seiler, E.R.D. ; Maitz, M.F. ; Villinger, A. ; Ehlers, P. ; Langer, P.
Title Total synthesis of dabigatran revisited; Synthesis of amidine-tosylated dabigatran
Date 19.12.2019
Number 58023
Abstract 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.
Journal Chemistry Select
Citation Chemistry Select 4 (2019) 13802-13805

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