Adventures in Drug-like Chemistry Space: From Oxetanes to Spiroazetidines and Beyond!

Authors

  • Mark Rogers-Evans F. Hoffmann-La Roche AG Pharma Research and Early Development Discovery Chemistry Roche Innovation Center, Basel Grenzacherstrasse CH-4070 Basel, Switzerland. mark.rogers-evans@roche.com
  • Henner Knust F. Hoffmann-La Roche AG Pharma Research and Early Development Discovery Chemistry Roche Innovation Center Basel Grenzacherstrasse CH-4070 Basel, Switzerland
  • Jean-Marc Plancher F. Hoffmann-La Roche AG Pharma Research and Early Development Discovery Chemistry Roche Innovation Center Basel Grenzacherstrasse CH-4070 Basel, Switzerland
  • Erick M. Carreira Laboratorium für Organische Chemie der ETH Vladimir Prelog Weg 3 CH-8093 Zürich, Switzerland
  • George Wuitschik Laboratorium für Organische Chemie der ETH Vladimir Prelog Weg 3 CH-8093 Zürich, Switzerland
  • Johannes Burkhard Laboratorium für Organische Chemie der ETH Vladimir Prelog Weg 3 CH-8093 Zürich, Switzerland
  • Dong B. Li Laboratorium für Organische Chemie der ETH Vladimir Prelog Weg 3 CH-8093 Zürich, Switzerland
  • Carine Guérot Laboratorium für Organische Chemie der ETH Vladimir Prelog Weg 3 CH-8093 Zürich, Switzerland

DOI:

https://doi.org/10.2533/chimia.2014.492

Keywords:

Chemistry and biology space, Compact modules, Oxetanes, Shape diversity, Spiroazetidines

Abstract

Recently we have documented research efforts aimed at new classes of oxetanes as well as spiroheteroalicyclic ring systems (which we have termed 'Compact Modules') designed to expand the palette of tailored module scaffolds available to medicinal chemists, which constitute an important role for synthetic chemistry in the drug discovery process. An essential component for this process is to provide access to specific molecular topologies with functional group diversity, essential for generating leads that discriminate among biological targets, therefore promoting selectivity and enhancing the safety profile of the final clinical candidates.

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Published

2014-08-27