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 …

Aryl transfer strategies mediated by photoinduced electron transfer

AR Allen, EA Noten, CRJ Stephenson - Chemical reviews, 2021 - ACS Publications
Radical aryl migrations are powerful techniques to forge new bonds in aromatic compounds.
The growing popularity of photoredox catalysis has led to an influx of novel strategies to …

A general organocatalytic system for electron donor–acceptor complex photoactivation and its use in radical processes

E de Pedro Beato, D Spinnato, W Zhou… - Journal of the …, 2021 - ACS Publications
We report herein a modular class of organic catalysts that, acting as donors, can readily form
photoactive electron donor–acceptor (EDA) complexes with a variety of radical precursors …

Recent advances in minisci‐type reactions

RSJ Proctor, RJ Phipps - Angewandte Chemie International …, 2019 - Wiley Online Library
Reactions that involve the addition of carbon‐centered radicals to basic heteroarenes,
followed by formal hydrogen atom loss, have become widely known as Minisci‐type …

Recent Advances in Photoredox‐Mediated Radical Conjugate Addition Reactions: An Expanding Toolkit for the Giese Reaction

AL Gant Kanegusuku, JL Roizen - … Chemie International Edition, 2021 - Wiley Online Library
Photomediated Giese reactions are at the forefront of radical chemistry, much like the
classical tin‐mediated Giese reactions were nearly forty years ago. With the global …

Installing the “magic methyl”–C–H methylation in synthesis

D Aynetdinova, MC Callens, HB Hicks… - Chemical Society …, 2021 - pubs.rsc.org
The selective and efficient C–H methylation of sp2 and sp3 carbon centres has become a
powerful transformation in the synthetic toolbox. Due to the potential for profound changes to …

Catalytic enantioselective Minisci-type addition to heteroarenes

RSJ Proctor, HJ Davis, RJ Phipps - Science, 2018 - science.org
Basic heteroarenes are a ubiquitous feature of pharmaceuticals and bioactive molecules,
and Minisci-type additions of radical nucleophiles are a leading method for their elaboration …

C H Bond Functionalization: Emerging Synthetic Tools for Natural Products and Pharmaceuticals

J Yamaguchi, AD Yamaguchi… - Angewandte Chemie …, 2012 - Wiley Online Library
The direct functionalization of C H bonds in organic compounds has recently emerged as a
powerful and ideal method for the formation of carbon–carbon and carbon–heteroatom …

Enantioselective C2–H alkylation of pyridines with 1, 3-dienes via Ni–Al bimetallic catalysis

JF Li, D Pan, HR Wang, T Zhang, Y Li… - Journal of the …, 2022 - ACS Publications
A chiral phosphine oxide-ligated Ni–Al bimetallic catalyst was used to realize an
enantioselective C2–H alkylation of pyridines without the need of a C2-block. A wide range …

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 …