Literature DB >> 28510279

1-Substituted 2-Azaspiro[3.3]heptanes: Overlooked Motifs for Drug Discovery.

Alexander A Kirichok1, Iryna Shton1, Maria Kliachyna1, Iryna Pishel1, Pavel K Mykhailiuk2,1.   

Abstract

The 2-substituted piperidine core is found in drugs (18 FDA-approved drugs), however, their spirocyclic analogues remain unknown. Described here is the synthesis of spirocyclic analogues for 2-substituted piperidines and a demonstration of their validation in drug discovery.
© 2017 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.

Entities:  

Keywords:  drug discovery; heterocycles; small rings; spirocycles; synthetic methods

Mesh:

Substances:

Year:  2017        PMID: 28510279     DOI: 10.1002/anie.201703801

Source DB:  PubMed          Journal:  Angew Chem Int Ed Engl        ISSN: 1433-7851            Impact factor:   15.336


  5 in total

1.  Palladium-Catalyzed Access to Benzocyclobutenone-Derived Ketonitrones via C(sp2)-H Functionalization.

Authors:  Jakub Brześkiewicz; Rafał Loska
Journal:  Org Lett       Date:  2022-05-25       Impact factor: 6.072

Review 2.  Put a ring on it: application of small aliphatic rings in medicinal chemistry.

Authors:  Matthias R Bauer; Paolo Di Fruscia; Simon C C Lucas; Iacovos N Michaelides; Jennifer E Nelson; R Ian Storer; Benjamin C Whitehurst
Journal:  RSC Med Chem       Date:  2021-01-07

3.  Strain-Release Driven Spirocyclization of Azabicyclo[1.1.0]butyl Ketones.

Authors:  Jasper L Tyler; Adam Noble; Varinder K Aggarwal
Journal:  Angew Chem Int Ed Engl       Date:  2021-04-16       Impact factor: 15.336

4.  Oxa-spirocycles: synthesis, properties and applications.

Authors:  Kateryna Fominova; Taras Diachuk; Dmitry Granat; Taras Savchuk; Vladyslav Vilchynskyi; Oleksiy Svitlychnyi; Vladyslav Meliantsev; Igor Kovalchuk; Eduard Litskan; Vadym V Levterov; Valentyn R Badlo; Ruslan I Vaskevych; Alla I Vaskevych; Andrii V Bolbut; Volodymyr V Semeno; Rustam Iminov; Kostiantyn Shvydenko; Anastasiia S Kuznetsova; Yurii V Dmytriv; Daniil Vysochyn; Vasyl Ripenko; Andrei A Tolmachev; Olexandra Pavlova; Halyna Kuznietsova; Iryna Pishel; Petro Borysko; Pavel K Mykhailiuk
Journal:  Chem Sci       Date:  2021-07-27       Impact factor: 9.825

5.  1,2-Difunctionalized bicyclo[1.1.1]pentanes: Long-sought-after mimetics for ortho/meta-substituted arenes.

Authors:  Jin-Xin Zhao; Yu-Xuan Chang; Chi He; Benjamin J Burke; Michael R Collins; Matthew Del Bel; Jeff Elleraas; Gary M Gallego; T Patrick Montgomery; James J Mousseau; Sajiv K Nair; Matthew A Perry; Jillian E Spangler; Julien C Vantourout; Phil S Baran
Journal:  Proc Natl Acad Sci U S A       Date:  2021-07-13       Impact factor: 11.205

  5 in total

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