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Spirocycles as Rigidified sp3-Rich Scaffolds for a Fragment Collection.

Accepted version
Peer-reviewed

Change log

Authors

Sveiczer, Attila 
North, Andrew JP 
Mateu, Natalia 
Kidd, Sarah L 
Sore, Hannah F 

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.

Description

Keywords

3405 Organic Chemistry, 34 Chemical Sciences

Journal Title

Org Lett

Conference Name

Journal ISSN

1523-7060
1523-7052

Volume Title

21

Publisher

American Chemical Society (ACS)

Rights

All rights reserved
Sponsorship
Engineering and Physical Sciences Research Council (EP/P020291/1)
European Commission (626191)