[HTML][HTML] Late-stage C–H functionalization offers new opportunities in drug discovery

L Guillemard, N Kaplaneris, L Ackermann… - Nature Reviews …, 2021 - nature.com
Over the past decade, the landscape of molecular synthesis has gained major impetus by
the introduction of late-stage functionalization (LSF) methodologies. C–H functionalization …

Carbon–Carbon Bond Cleavage for Late-Stage Functionalization

YF Liang, M Bilal, LY Tang, TZ Wang, YQ Guan… - Chemical …, 2023 - ACS Publications
Late-stage functionalization (LSF) introduces functional group or structural modification at
the final stage of the synthesis of natural products, drugs, and complex compounds. It is …

[HTML][HTML] Regioselective aliphatic C–H functionalization using frustrated radical pairs

Z Lu, M Ju, Y Wang, JM Meinhardt… - Nature, 2023 - nature.com
Abstract Frustrated Lewis pairs (FLPs) are well documented for the activation of small
molecules such as dihydrogen and carbon dioxide,,–. Although canonical FLP chemistry is …

Diversification of aliphatic C–H bonds in small molecules and polyolefins through radical chain transfer

TJ Fazekas, JW Alty, EK Neidhart, AS Miller… - Science, 2022 - science.org
The ability to selectively introduce diverse functionality onto hydrocarbons is of substantial
value in the synthesis of both small molecules and polymers. Herein, we report an approach …

Green chemistry meets medicinal chemistry: a perspective on modern metal-free late-stage functionalization reactions

JD Lasso, DJ Castillo-Pazos, CJ Li - Chemical Society Reviews, 2021 - pubs.rsc.org
The progress of drug discovery and development is paced by milestones reached in organic
synthesis. In the last decade, the advent of late-stage functionalization (LSF) reactions has …

Skeletal editing of (hetero) arenes using carbenes

Z Liu, P Sivaguru, Y Ning, Y Wu… - Chemistry–A European …, 2023 - Wiley Online Library
Abstract (Hetero) arenes continue to prove their indispensability in pharmaceuticals,
materials science, and synthetic chemistry. As such, the controllable modification of …

[HTML][HTML] Strategic application of C–H oxidation in natural product total synthesis

I Bakanas, RF Lusi, S Wiesler… - Nature Reviews …, 2023 - nature.com
The oxidation of unactivated C–H bonds has emerged as an effective tactic in natural
product synthesis and has altered how chemists approach the synthesis of complex …

Skeletal editing: interconversion of arenes and heteroarenes

BW Joynson, LT Ball - Helvetica Chimica Acta, 2023 - Wiley Online Library
Skeletal editing involves making specific point‐changes to the core of a molecule through
the selective insertion, deletion or exchange of atoms. It thus represents a potentially …

Rational design of bioinspired catalysts for selective oxidations

L Vicens, G Olivo, M Costas - ACS Catalysis, 2020 - ACS Publications
Recognizing Nature's unique ability to perform challenging oxygenation reactions with
exquisite selectivity parameters at iron-dependent oxygenases, chemists have long sought …

Transition Metal-Catalyzed Direct Stereoselective Oxygenations of C(sp3)–H Groups

KP Bryliakov - ACS Catalysis, 2023 - ACS Publications
Designing catalytic approaches to deliberate and selective C–H activation was listed by
Bergman among the “Holy Grails” of synthetic chemistry in 1995, and continues to be a hot …