Electrochemical late-stage functionalization

Y Wang, S Dana, H Long, Y Xu, Y Li… - Chemical …, 2023 - ACS Publications
Late-stage functionalization (LSF) constitutes a powerful strategy for the assembly or
diversification of novel molecular entities with improved physicochemical or biological …

Emerging building blocks for medicinal chemistry: recent synthetic advances

OO Grygorenko, DM Volochnyuk… - European Journal of …, 2021 - Wiley Online Library
Current medicinal chemistry relies heavily on the quality of building blocks, ie reagents used
to introduce chemical diversity into the target molecules. The last decade witnessed an …

Electrochemical C–H phosphorylation of arenes in continuous flow suitable for late-stage functionalization

H Long, C Huang, YT Zheng, ZY Li, LH Jie… - Nature …, 2021 - nature.com
The development of efficient and sustainable methods for carbon-phosphorus bond
formation is of great importance due to the wide application of organophosphorus …

A close-up look at the chemical space of commercially available building blocks for medicinal chemistry

Y Zabolotna, DM Volochnyuk… - Journal of chemical …, 2021 - ACS Publications
The ability to efficiently synthesize desired compounds can be a limiting factor for chemical
space exploration in drug discovery. This ability is conditioned not only by the existence of …

N-Trifluoromethyl Amines and Azoles: An Underexplored Functional Group in the Medicinal Chemist's Toolbox

S Schiesser, H Chepliaka, J Kollback… - Journal of Medicinal …, 2020 - ACS Publications
Introducing trifluoromethyl groups is a common strategy to improve the properties of
biologically active compounds. However, N-trifluoromethyl moieties on amines and azoles …

Design and Synthesis of Sulfanilamide Aminophosphonates as Novel Antibacterial Agents towards Escherichia coli

J Wang, MF Ansari, JM Lin… - Chinese Journal of …, 2021 - Wiley Online Library
Main observation and conclusion The limit ability of traditional antibiotics to treat drug
resistant bacteria calls for new therapeutic alternatives. A class of unique sulfanilamide …

Asymmetric Hydrophosphinylation of Alkynes: Facile Access to Axially Chiral Styrene‐Phosphines

B Cai, Y Cui, J Zhou, YB Wang, L Yang… - Angewandte Chemie …, 2023 - Wiley Online Library
A Cu/CPA co‐catalytic system has been developed for achieving the direct
hydrophosphinylation of alkynes with phosphine oxides in delivering novel axially chiral …

Discovery of SY-5609: a selective, noncovalent inhibitor of CDK7

JJ Marineau, KB Hamman, S Hu… - Journal of Medicinal …, 2021 - ACS Publications
CDK7 has emerged as an exciting target in oncology due to its roles in two important
processes that are misregulated in cancer cells: cell cycle and transcription. This report …

An update on late-stage functionalization in today's drug discovery

AP Montgomery, JM Joyce, JJ Danon… - Expert Opinion on Drug …, 2023 - Taylor & Francis
Introduction Late-stage functionalization (LSF) allows for the introduction of new chemical
groups toward the end of a synthetic sequence, which means new molecules can be rapidly …

gem‐Heteroatom‐Substituted Fluoroalkenes as Mimics of Amide Derivatives or Phosphates: A Comprehensive Review

S Morand, P Jubault, JP Bouillon… - … A European Journal, 2021 - Wiley Online Library
Abstract gem‐Heteroatom‐substituted fluoroalkenes have received little attention despite
their great potential in medicinal chemistry or in fine chemistry. Indeed, due to the electronic …