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Synthesis of sp3-rich heterocyclic frameworks by a divergent synthesis strategy.


ABSTRACT: Fragment-based lead discovery (FBLD) often relies on flat, aromatic compounds which display undesirable physicochemical properties with limited exit vectors for fragment growth. Herein, we report concise synthetic strategies to sp3-rich heterocyclic fragments encompassing polar exit vectors poised for fragment-to-lead (F2L) development.

SUBMITTER: Mortensen KT 

PROVIDER: S-EPMC10246434 | biostudies-literature | 2023 Jun

REPOSITORIES: biostudies-literature

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Synthesis of sp<sup>3</sup>-rich heterocyclic frameworks by a divergent synthesis strategy.

Mortensen Kim T KT   Wong Denedy S Y DSY   King Thomas A TA   Sore Hannah F HF   Spring David R DR  

Organic & biomolecular chemistry 20230607 22


Fragment-based lead discovery (FBLD) often relies on flat, aromatic compounds which display undesirable physicochemical properties with limited exit vectors for fragment growth. Herein, we report concise synthetic strategies to sp<sup>3</sup>-rich heterocyclic fragments encompassing polar exit vectors poised for fragment-to-lead (F2L) development. ...[more]

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