Electrochemical late-stage functionalization
Late-stage functionalization (LSF) constitutes a powerful strategy for the assembly or
diversification of novel molecular entities with improved physicochemical or biological …
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 …
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 …
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 …
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 …
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 …
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 …
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 …
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 …
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 …
their great potential in medicinal chemistry or in fine chemistry. Indeed, due to the electronic …