Design and optimization of selective serotonin re-uptake inhibitors with high synthetic accessibility. Part 1

  • Bioorg Med Chem Lett. 2009 Apr 15;19(8):2329-32. doi: 10.1016/j.bmcl.2009.02.054.
Mark Andrews  1 ,  Alan Brown ,  Jean-Yves Chiva ,  David Fradet ,  David Gordon ,  Mark Lansdell ,  Malcolm MacKenny
Affiliations
  • 1. Discovery Chemistry, Pfizer Global Research and Development, Sandwich, United Kingdom.
PMID: 19282174 DOI: 10.1016/j.bmcl.2009.02.054
Abstract

The reported selective serotonin Re-uptake Inhibitor Litoxetine was used as the starting point in the design of a range of potential SSRIs with high ease of synthetic accessibility. Preparation and subsequent optimization yielded a range of potent and highly selective SSRIs.