Abstract
The re-emergence, in the recent years, of cyclooxygenase as a biological target in therapeutic areas other than inflammation is likely to require new optimized leads, particularly suited for the requirements of specific drug development programs. We developed a convenient synthesis of the known imidazole-based selective COX-2 inhibitors bearing primary sulphonamide and methyl sulfone substituents, via Pd-catalyzed imidazoline N-arylation as a key step, followed by dehydrogenation.
Keywords: Buchwald-Hartwig arylation, 2-imidazolines, dehydrogenation, sulphonamide, methyl sulfone, protecting groups, cyclooxygenase inhibitors.
Letters in Organic Chemistry
Title:Pd-Catalyzed N-arylation of 2-imidazolines Provides Convenient Access to Selective Cyclooxygenase-2 Inhibitors
Volume: 10 Issue: 4
Author(s): Mikhail Krasavin
Affiliation:
Keywords: Buchwald-Hartwig arylation, 2-imidazolines, dehydrogenation, sulphonamide, methyl sulfone, protecting groups, cyclooxygenase inhibitors.
Abstract: The re-emergence, in the recent years, of cyclooxygenase as a biological target in therapeutic areas other than inflammation is likely to require new optimized leads, particularly suited for the requirements of specific drug development programs. We developed a convenient synthesis of the known imidazole-based selective COX-2 inhibitors bearing primary sulphonamide and methyl sulfone substituents, via Pd-catalyzed imidazoline N-arylation as a key step, followed by dehydrogenation.
Export Options
About this article
Cite this article as:
Krasavin Mikhail, Pd-Catalyzed N-arylation of 2-imidazolines Provides Convenient Access to Selective Cyclooxygenase-2 Inhibitors, Letters in Organic Chemistry 2013; 10 (4) . https://dx.doi.org/10.2174/1570178611310040002
DOI https://dx.doi.org/10.2174/1570178611310040002 |
Print ISSN 1570-1786 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6255 |
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Meet Our Editorial Board Member
CNS & Neurological Disorders - Drug Targets Preface- Novel Targets for CNS Anti-Inflammatory Drug Development Interfering with Eicosanoid Formation
Current Medicinal Chemistry - Anti-Inflammatory & Anti-Allergy Agents FKBP Ligands as Novel Therapeutics for Neurological Disorders
Mini-Reviews in Medicinal Chemistry In vitro and in vivo Evaluation of Antitumor Drug-Loaded Aptamer Targeted Single-Walled Carbon Nanotubes System
Current Pharmaceutical Biotechnology Stem Cells Therapies in Basic Science and Translational Medicine: Current Status and Treatment Monitoring Strategies
Current Pharmaceutical Biotechnology Chitosan and Its Use in Design of Insulin Delivery System
Recent Patents on Drug Delivery & Formulation Advanced Neuroimaging Techniques in the Management of Glioblastoma Multiforme
Current Radiopharmaceuticals Potential of Photobiomodulation to Induce Differentiation of Adipose- Derived Mesenchymal Stem Cells into Neural Cells
Current Stem Cell Research & Therapy P2Y Receptors: Focus on Structural, Pharmacological and Functional Aspects in the Brain
Current Medicinal Chemistry Vasotrophic Regulation of Age-Dependent Hypoxic Cerebrovascular Remodeling
Current Vascular Pharmacology Reactive Astrocytes as Potential Manipulation Targets in Novel Cell Replacement Therapy of Parkinsons Disease
Current Drug Targets Mst1: Function and Mechanism in Brain and Myocardial Ischemia Reperfusion Injury
Current Neuropharmacology Mesenchymal Stem Cells as Mediators of Neural Differentiation
Current Stem Cell Research & Therapy Synthesis and Biological Applications of Triazole Derivatives – A Review
Mini-Reviews in Organic Chemistry Partial QSAR Analysis of Some Selected Natural Inhibitors of FAAH Suggests a Working Hypothesis for the Development of Endocannabinoid- Based Drugs
Current Drug Targets - CNS & Neurological Disorders Synthesis of Novel Aryl (4-Aryl-1H-Pyrrol-3-yl) (Thiophen-2-yl) Methanone Derivatives: Molecular Modelling, In Silico ADMET, Anti-Inflammatory and Anti-Ulcer Activities
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Major Highlights of the CAR-TCR Summit, Boston, 2016
Anti-Cancer Agents in Medicinal Chemistry Neuropharmacological Aspects of Crocus sativus L.: A Review of Preclinical Studies and Ongoing Clinical Research
CNS & Neurological Disorders - Drug Targets Physiology, Pharmacology and Pathophysiology of the pH Regulatory Transport Proteins NHE1 and NBCn1: Similarities, Differences, and Implications for Cancer Therapy
Current Pharmaceutical Design Basic Pharmacology of NMDA Receptors
Current Pharmaceutical Design