[HTML][HTML] The powerful symbiosis between synthetic and medicinal chemistry

S Schiesser, RJ Cox, W Czechtizky - Future Medicinal Chemistry, 2021 - Future Science
The discovery of innovative small-molecule drugs is a challenging endeavor. Medicinal
chemists need to continuously optimize the properties of bioactive compounds while at the …

Highly efficient and well-defined phosphinous acid-ligated Pd (II) precatalysts for Hirao cross-coupling reaction

LH Hong, WJ Feng, WC Chen, YC Chang - Dalton Transactions, 2023 - pubs.rsc.org
We report the synthesis of a new palladium complex (1a) bearing two different P-donors, di
(1-adamantyl) phosphinous acid and triphenylphosphine. A heteroleptic complex with a …

[HTML][HTML] Novel design of dual-action Pt (IV) anticancer pro-drugs based on cisplatin and derivatives of the tyrosine kinase inhibitors imatinib and nilotinib

DF Beirne, B Farkaš, C Donati, V Gandin, I Rozas… - Dalton …, 2023 - pubs.rsc.org
Tyrosine kinases (TKs) are emerging as important targets in cancer therapy and some of
their inhibitors, TKIs (eg imatinib and nilotinib), are FDA-approved drugs that are used as …

Studying Lipophilicity Trends of Phosphorus Compounds by 31P-NMR Spectroscopy: A Powerful Tool for the Design of P-Containing Drugs

I Columbus, L Ghindes-Azaria, R Chen… - Journal of Medicinal …, 2022 - ACS Publications
Systematically studying the lipophilicity of phosphorus compounds is of great importance for
many chemical and biological fields and particularly for medicinal chemistry. Here, we report …

γ-Amino phosphonates via the photocatalytic α-C–H alkylation of primary amines

JD Grayson, AJ Cresswell - Tetrahedron, 2021 - Elsevier
We report a simple photocatalytic protocol for the direct synthesis of γ-amino phosphonates
via the α-C–H alkylation of unprotected, aliphatic primary amines with diethyl …

[PDF][PDF] Secondary phosphine oxide-activated nickel catalysts for site-selective alkene isomerization and remote hydrophosphination

L Huang, EQ Lim, MJ Koh - Chem Catalysis, 2022 - cell.com
Catalytic systems that are readily modifiable to achieve olefin migration or remote
functionalization are highly sought after in chemical synthesis. Here, we show that the …

Synthesis of γ-Oxo-phosphonates via N-Heterocyclic Carbene-Catalyzed Acylphosphorylation of Alkenes

JN Mo, S Sun, H Xu, H Shu, J Zhao - Organic Letters, 2024 - ACS Publications
In this study, we present an N-heterocyclic carbene-catalyzed method for the radical
acylphosphorylation of alkenes. Electrochemical investigations were employed to identify an …

[HTML][HTML] Cobalt-or rhodium-catalyzed synthesis of 1, 2-dihydrophosphete oxides via C–H activation and formal phosphoryl migration

S Xu, R Mi, G Zheng, X Li - Chemical Science, 2024 - pubs.rsc.org
A highly stereo-and chemoselective intermolecular coupling of diverse heterocycles with
dialkynylphosphine oxides has been realized via cobalt/rhodium-catalyzed C–H bond …

Simple approach towards phosphorus-substituted spiro 1, 3, 4-thiadiazolines

M Kozlov, A Tyurin, A Dmitrenok, V Rusak, A Fedorov… - Tetrahedron, 2024 - Elsevier
This study reports the first general, practical, and facile synthesis of phosphorus-substituted
1, 3, 4-thiadiazolines starting from phosphorylthioformic acid hydrazides and ketones …

A Mild Synthesis of Aryl Triflates Enabling the Late‐Stage Modification of Drug Analogs and Complex Peptides

S Schiesser, J Ceklarz, J Kollback… - … A European Journal, 2023 - Wiley Online Library
We report the discovery of a straightforward protocol to convert phenols into the
corresponding aryl triflates using 1‐methyl‐3‐((trifluoromethyl) sulfonyl)‐1, 3‐dihydro‐2H …