4.6 Article

A Machine-Assisted Flow Synthesis of SR48692: A Probe for the Investigation of Neurotensin Receptor-1

Journal

CHEMISTRY-A EUROPEAN JOURNAL
Volume 19, Issue 24, Pages 7917-7930

Publisher

WILEY-V C H VERLAG GMBH
DOI: 10.1002/chem.201300696

Keywords

batch processes; flow chemistry; medicinal chemistry; organic chemistry; synthetic methods

Funding

  1. Pfizer
  2. Commonwealth Scholarship Commission
  3. EPSRC
  4. BP 1702 endowment
  5. Royal Society
  6. EPSRC [EP/F069685/1] Funding Source: UKRI
  7. Engineering and Physical Sciences Research Council [EP/F069685/1] Funding Source: researchfish

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Here we report the direct comparison of a conventional batch mode synthesis of Meclinertant (SR48692, 1), a neurotensin receptor-1 antagonist, with its machine-assisted flow chemistry alternative. By using these enabling tools, combined with solid-supported reagents and scavengers, many process advantages were observed. Care, however, must be taken not to convert these techniques into expensive solutions to problems that do not exist.

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