Issue 13, 2021

Emergent synthetic methods for the modular advancement of sp3-rich fragments

Abstract

Fragment-based drug discovery is an important and increasingly reliable technology for the delivery of clinical candidates. Notably, however, sp3-rich fragments are a largely untapped resource in molecular discovery, in part due to the lack of general and suitably robust chemical methods available to aid their development into higher affinity lead and drug compounds. This Perspective describes the challenges associated with developing sp3-rich fragments, and succinctly highlights recent advances in C(sp3)–H functionalisations of high potential value towards advancing fragment hits by ‘growing’ functionalised rings and chains from unconventional, carbon-centred vectors.

Graphical abstract: Emergent synthetic methods for the modular advancement of sp3-rich fragments

Article information

Article type
Perspective
Submitted
09 jan 2021
Accepted
28 fev 2021
First published
02 mar 2021
This article is Open Access

All publication charges for this article have been paid for by the Royal Society of Chemistry
Creative Commons BY-NC license

Chem. Sci., 2021,12, 4646-4660

Emergent synthetic methods for the modular advancement of sp3-rich fragments

M. J. Caplin and D. J. Foley, Chem. Sci., 2021, 12, 4646 DOI: 10.1039/D1SC00161B

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