Spirocycles as Rigidified sp3-Rich Scaffolds for a Fragment Collection.
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Peer-reviewed
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Abstract
Novel divergent methodology to access sp3-rich spirocyclic fragments is reported. First, a robust modular synthesis of bis-alkene amino ester building blocks was developed. Three different carbocycles and six heterocycles were then constructed to assemble eight spirocycles. Importantly, strategic exit vectors were incorporated within each scaffold to aid fragment growth and were elaborated via chemical modifications. Finally, computational methods demonstrate higher levels of rigidity, three-dimensionality, and structural diversity of the library compared to a commercial collection.
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Keywords
3405 Organic Chemistry, 34 Chemical Sciences
Journal Title
Org Lett
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Journal ISSN
1523-7060
1523-7052
1523-7052
Volume Title
21
Publisher
American Chemical Society (ACS)
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All rights reserved
Sponsorship
Engineering and Physical Sciences Research Council (EP/P020291/1)
European Commission (626191)
European Commission (626191)