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Academia / Industry Collaborations towards the Functionalization of Aryl Azoles

Chimia, 2024-03, Vol.78 (3), p.104-107 [Peer Reviewed Journal]

Copyright 2024 Simon Wagschal, Diego Broggini. License: This work is licensed under a Creative Commons Attribution 4.0 International License. ;ISSN: 0009-4293 ;EISSN: 2673-2424 ;DOI: 10.2533/chimia.2024.104 ;PMID: 38547010

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  • Title:
    Academia / Industry Collaborations towards the Functionalization of Aryl Azoles
  • Author: Wagschal, Simon ; Broggini, Diego
  • Subjects: Aryl azoles ; Metalation ; Milvexian ; Triazoles
  • Is Part Of: Chimia, 2024-03, Vol.78 (3), p.104-107
  • Description: Aryl azoles can be found in numerous active pharmaceutical ingredients (APIs). Milvexian is a Factor Xia inhibitor currently in phase III for the treatment of thrombotic events containing an ortho-substituted 1-aryl-1H-1,2,3-triazole moiety. During the process development of Milvexian, we assessed multiple approaches for the preparation of 4-chloro-1,2,3-triazole, intermediate 1. In this review article, we will detail how we initiated several academic collaborations to speed up the selection of the best synthesis for commercial manufacturing. Ultimately, those results not only helped us to achieve our goal but yielded general methodologies for the functionalization of azoles that extended even beyond our initial scope.
  • Publisher: Switzerland: Swiss Chemical Society
  • Language: English;German
  • Identifier: ISSN: 0009-4293
    EISSN: 2673-2424
    DOI: 10.2533/chimia.2024.104
    PMID: 38547010
  • Source: DOAJ Directory of Open Access Journals
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