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 …
functionalization, has revolutionized the field of organic synthesis. Over the past decade …
Aryl transfer strategies mediated by photoinduced electron transfer
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 …
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 …
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 …
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 …
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 …
powerful transformation in the synthetic toolbox. Due to the potential for profound changes to …
Catalytic enantioselective Minisci-type addition to heteroarenes
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 …
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 …
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 …
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
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 very last steps of the synthesis. LSF has the potential to speed up the preparation of …