Late-stage functionalization for improving drug-like molecular properties

NJ Castellino, AP Montgomery, JJ Danon… - Chemical …, 2023 - ACS Publications
The development of late-stage functionalization (LSF) methodologies, particularly C–H
functionalization, has revolutionized the field of organic synthesis. Over the past decade …

The medicinal chemist's toolbox for late stage functionalization of drug-like molecules

T Cernak, KD Dykstra, S Tyagarajan… - Chemical Society …, 2016 - pubs.rsc.org
The advent of modern C–H functionalization chemistries has enabled medicinal chemists to
consider a synthetic strategy, late stage functionalization (LSF), which utilizes the C–H …

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 …

An overview of late-stage functionalization in today's drug discovery

M Moir, JJ Danon, TA Reekie… - Expert Opinion on Drug …, 2019 - Taylor & Francis
Introduction: Late-stage functionalization (LSF) can introduce important chemical groups in
the very last steps of the synthesis. LSF has the potential to speed up the preparation of …

The emergence of the C–H functionalization strategy in medicinal chemistry and drug discovery

R Jana, HM Begam, E Dinda - Chemical Communications, 2021 - pubs.rsc.org
Owing to the market competitiveness and urgent societal need, an optimum speed of drug
discovery is an important criterion for successful implementation. Despite the rapid ascent of …

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 …

Late-stage functionalization

J Börgel, T Ritter - Chem, 2020 - cell.com
The term late-stage functionalization (LSF) is recent but is now frequently used in the field of
organic methodology development to describe transformations on complex molecules. Such …

Synthetic approaches to the new drugs approved during 2015

AC Flick, HX Ding, CA Leverett… - Journal of medicinal …, 2017 - ACS Publications
New drugs introduced to the market every year represent privileged structures for particular
biological targets. These new chemical entities (NCEs) provide insight into molecular …

Late stage C–H functionalization via chalcogen and pnictogen salts

CB Kelly, R Padilla-Salinas - Chemical Science, 2020 - pubs.rsc.org
Late-stage functionalization (LSF) of heteroarenes can dramatically accelerate SAR studies
by enabling the installation of functional groups that would otherwise complicate a synthetic …

A perspective on late-stage aromatic C–H bond functionalization

L Zhang, T Ritter - Journal of the American Chemical Society, 2022 - ACS Publications
Late-stage functionalization of C–H bonds (C–H LSF) can provide a straightforward
approach to the efficient synthesis of functionalized complex molecules. However, C–H LSF …