The oxidative debenzylation of N-benzyl amides and O-benzyl ethers was promoted with high efficiency by a bromo radical formed through the oxidation of bromide from alkali metal bromide under mild conditions. This reaction provided the corresponding amides from N-benzyl amides and carbonyl compounds from O-benzyl ethers in high yields.
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http://dx.doi.org/10.1021/ol501703y | DOI Listing |
Int J Pharm
January 2025
Departamento de Farmacología, Farmacia y Tecnología Farmacéutica, I+D Farma (GI-1645), Faculty of Pharmacy, iMATUS, and Health Research Institute of Santiago de Compostela (IDIS), Universidade de Santiago de Compostela, Santiago de Compostela 15782, Spain. Electronic address:
Heme oxygenase-1 (HO-1) has been identified as a potential new target in anticancer therapy, being overexpressed in different tumors and crucial for cell proliferation. Advances in the development of specific HO-1 inhibitors should support the understanding of controlling HO-1 activity as antitumoral strategies, opening the path for future therapeutic applications. In the present study, small series of new HO-1 inhibitors were synthesized by joining a butylimidazolic pharmacophore together with a hydrophobic moiety spaced by a 2-oxybenzamide central linker.
View Article and Find Full Text PDFChem Commun (Camb)
October 2024
Department of Chemistry and Chemical Biology, Northeastern University, Boston, MA 02115, USA.
RSC Adv
September 2024
Bioinspired & Biomimetic Inorganic Chemistry Lab, Department of Chemistry, National Institute of Technology Calicut Kozhikode Kerala 673601 India
Selective functionalisation of hydrocarbons using transition metal complexes has evoked significant research interest in industrial chemistry. However, selective oxidation of unactivated aliphatic C-H bonds is challenging because of the high bond dissociation energies. Herein, we report the synthesis, characterisation and catalytic activity of nickel(ii) complexes ([Ni(L1-L3)(OH)](ClO) (1-3)) of monoamidate tetradentate ligands [L1: 2-(bis(pyridin-2-ylmethyl)amino)--phenylacetamide, L2: 2-(bis(2-pyridin-2-ylmethyl)amino)--(naphthalen-1-yl)acetamide, L3: -benzyl-2-(bis(pyridin-2-ylmethyl)amino)acetamide] in selective oxidation of cycloalkanes using -CPBA as the oxidant.
View Article and Find Full Text PDFEur J Med Chem
October 2024
Department of Medicinal Chemistry, School of Pharmacy, Fudan University, No. 826 Zhangheng Road, Shanghai, 201203, China. Electronic address:
The effective management of moderate to severe pain often relies on the use of analgesic agents. However, the widespread utility of these medications is hindered by the occurrence of several undesirable side effects. In light of this challenge, there is growing interest in the development of κ opioid receptor (KOR) agonists, which have shown promise in mitigating these adverse effects.
View Article and Find Full Text PDFOrg Lett
July 2024
Department of Applied Chemistry, Graduate School of Engineering, Osaka University, Suita, Osaka 565-0871, Japan.
In this study, we present the catalytic conversion of benzylamides featuring an ortho alkynyl moiety into 1-acylisoindole derivatives via a 1,2-acyl shift. Remarkably, this transformation proceeds without the need for transition-metal catalysts; instead, KOBu alone serves as the catalyst. This method enables the efficient synthesis of isoindoles from easily accessible amides with an atom economy of 100%.
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