[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 …
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 …
(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
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 …
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 …
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 …
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 …
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 …
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 …
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 …
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 …
corresponding aryl triflates using 1‐methyl‐3‐((trifluoromethyl) sulfonyl)‐1, 3‐dihydro‐2H …