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Chapter 18

Accessing Novel Molecular Motifs and Monomers

With increased emphasis in the pharmaceutical industry on rapid progression of projects to drug candidates, parallel synthesis plays a vital role. The need for a diverse and streamlined collection of building blocks, or monomers, is paramount in rapid synthesis and identification of drug like molecules that can be developed to drug candidates. Herein, we describe how Pfizer used a multi-faceted approach to craft its monomer collection to address these challenges. This included development of a “Tier 1” set that focused on diversity and physical properties, increased monomer access through use of in situ monomer synthesis, identifying a set of monomers for rapid SAR optimization, development of multistep library protocols and creative and novel core synthesis. The chapter will also show how recent developments in academic research can be leveraged to diversify monomer collections by adding new structural motifs that enable new design space. In particular, we will show how new synthetic methods to prepare novel spirocyclic systems, diverse oxetanes, and various fluorinated monomers can be used in the expansion of building block collections. Finally, we provide our view of the future of monomer design.

Publication details

Print publication date
01 Aug 2016
Copyright year
2016
Print ISBN
978-1-78262-786-9
PDF eISBN
978-1-78262-791-3
ePub eISBN
978-1-78262-792-0

From the book series:
Drug Discovery