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- Volume 15, Issue 2, 2018
Current Organic Synthesis - Volume 15, Issue 2, 2018
Volume 15, Issue 2, 2018
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Strategies for the Synthesis of Hydroxamic Acids
Authors: Ankit Ganeshpurkar, Devendra Kumar and Sushil K. SinghBackground: Hydroxamic acids are a major class of organic compounds. They have a wide variety of pharmacological actions in targeting cancers, cardiovascular diseases, HIV, Alzheimer's disease, Malaria, Allergic diseases. Objective: The present review focuses on the chemistry of conventional and non-conventional routes for the synthesis of hydroxamic acids reported till date. Conclusion: The hydroxamic acids are Read More
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An Overview on Chemistry and Biological Importance of Pyrrolidinone
Background: Pyrrolidinone is a five membered heterocyclic ring that is a versatile lead compound for designing powerful bioactive agents. Pyrrolidinone nucleus is one of the most important heterocyclic compound indicating notable pharmaceutical effects. Many procedures for the preparation of pyrrolidinone and also their various reactions offer great scope in the field of medicinal chemistry. This fascinating group Read More
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Synthesis and Biological Evaluations of Organoruthenium Scaffolds: A Comprehensive Update
Authors: Ashaparna Mondal and Priyankar PairaBackground: Currently ruthenium complexes are immerging as effective anticancer agents due to their less toxicity, better antiproliferative and antimetastatic activity, better stability in cellular environment and most importantly variable oxidation and co-ordination states of ruthenium allows binding this molecule with a variety of ligands. So in past few years researchers have shifted their interest towards organoruthenium co Read More
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Pd Catalyzed N1/N4 Arylation of Piperazine for Synthesis of Drugs, Biological and Pharmaceutical Targets: An Overview of Buchwald Hartwig Amination Reaction of Piperazine in Drug Synthesis
Authors: Vaibhav Mishra and Tejpal S. ChundawatBackground: Substituted piperazine heterocycles are among the most significant structural components of pharmaceuticals. N1/N4 substituted piperazine containing drugs and biological targets are ranked 3rd in the top most frequent nitrogen heterocycles in U.S. FDA approved drugs. The high demand of N1/N4 substituted piperazine containing biologically active compounds and U.S. FDA approved drugs, has prompted the Read More
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Enantioselective Syntheses of Flavonoid Diels-Alder Natural Products: A Review
Authors: Shah B. Nasir, Noorsaadah Abd Rahman and Chin Fei CheeBackground: The Diels-Alder reaction has been widely utilised in the syntheses of biologically important natural products over the years and continues to greatly impact modern synthetic methodology. Recent discovery of chiral organocatalysts, auxiliaries and ligands in organic synthesis has paved the way for their application in Diels-Alder chemistry with the goal to improve efficiency as well as stereochemistry. Objective: Read More
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(±)-3,5-Bis(substitutedmethyl)pyrrolidines: Application to the Synthesis of Analogues of glycine-L-proline-L-glutamic Acid (GPE)
Authors: Joana F. da Costa, Xerardo Garcia-Mera, David Silva Poceiro and Olga CaamanoBackiground: Alzheimer's disease is a fatal, complex, neurodegenerative disease over 46 million people live with dementia in the world characterized by the presence of plaques containing β-amyloid and neuronal loss. The GPE acts as a survival factor against β-amyloid insult in brain and suggests a possible new therapeutic strategy for the treatment of Central Nervous System injuries and neurodegenerative disorders Read More
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Synthesis and Antitumor Evaluation of Novel N-substituted Norcantharidin Imidazolium Derivatives
Authors: Rong-Rong Sun, Jia-Hui Guo, Cui Yang, Li-Juan Yang and Chao HuangAims and Objectives: Cantharidin is a terpenoid with a high vesicant potency isolated from Mylabris caraganae and various other insects, which originates from the Chinese traditional medicine and has a long history of use as antiproliferative agent. Modified cantharidin derivatives are researched for retainable antitumor activities and lower toxicity. And imidazolium salt is an important building block in drug discovery wit Read More
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Expeditious Preparation of N-Fmoc 2-Aminoethanesulfonyl Chlorides with Functionalized 1-Substituents
Authors: Kheira Haiouani, Xingpeng Chen and Jiaxi XuAim and Objective: [(9H-Fluoren-9-yl)methoxy]carbonyl (Fmoc)-protected 2-aminoethanesulfonyl chlorides with various functionalized 1-substituents may be of use as building blocks for the Fmoc strategic synthesis of sulfonopeptides. Material and Method: Fmoc-protected 2-aminoethanesulfonyl chlorides with different functionalized 1- substituents were synthesized via radical addition of N-Fmoc allylamine an Read More
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The Discovery of Ultrasound Irradiation as a Useful Tool for Accelerating Petasis Three-component Reaction: Synthesis of α-Arylglycines
Authors: Fan Yun, Chunhui Cheng, Jingxuan Li, Pingwah Tang and Qipeng YuanAim and Objective: α-Arylglycines belong to an important class of non-proteinogenic amino acids. Petasis 3-component, one-pot reaction lends itself to be suitable for the synthesis of α-Arylglycines. Because of the low reactivity, Petasis reaction requires long reaction time. Our objective is to use ultrasound irradiation to accelerate this versatile Petasis' synthesis of α-Arylglycines. Materials and Methods: Ultrasound irradiation as a Read More
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One Pot Synthesis of Novel Substituted 2',4'-Dihydrospiro[chroman-2,3'-pyrazol]-4-one Derivatives
Aim and Objective: In the work, we have successfully presented a synthetic route for the synthesis of novel 2',4'-dihydrospiro[chroman-2,3'-pyrazol]-4-one derivatives via one pot multicomponent approach. Material and Method: Substituted 2',4'-dihydrospiro[chroman-2,3'-pyrazol]-4-one were prepared through cascade three-component condensation of ortho-hydroxyacetophenone, β-ketoester, hydrazine in the presence Read More
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Design, Synthesis and Docking study of Novel Imidazolyl Pyrazolopyridine Derivatives as Antitumor Agents Targeting MCF7 Cell Line
Authors: Mohamed A. El-Borai, Mohamed K. Awad, H.F. Rizk and Faten M. AtlamAim and Objective: Pyrazolo pyridine skeleton is an interesting class of heterocycles due to its diverse biological properties including antitumor, antioxidant and antibacterial activities. The objective of this work was established in vitro antiproliferative activities against MCF-7 (breast cancer) human cell lines for of the synthesized compounds IIIa-e. The effect of the molecular and electronic structures on the biological activity Read More
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Synthesis of New α-Amino Phosphonates Containing 3-Amino-4(3H) Quinazolinone Moiety as Anticancer and Antimicrobial Agents: DFT, NBO, and Vibrational Studies
Authors: Mohamed K. Awad, Mahmoud F. Abdel-Aal, Faten M. Atlam and Hend A. HekalAim and Objective: Synthesis of new α-aminophosphonates containing quinazoline moiety through Kabachnik-Fields reaction in the presence of copper triflate catalyst [32], followed by studying their antimicrobial activities and in vitro anticancer activities against liver carcinoma cell line (HepG2) with the hope that new anticancer agents could be developed. Also, the quantum chemical calculations are performed using de Read More
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Volumes & issues
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Volume 22 (2025)
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Volume 21 (2024)
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Volume 20 (2023)
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Volume 19 (2022)
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Volume 18 (2021)
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Volume 17 (2020)
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Volume 16 (2019)
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Volume 15 (2018)
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Volume 14 (2017)
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Volume 13 (2016)
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Volume 12 (2015)
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Volume 11 (2014)
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Volume 10 (2013)
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Volume 9 (2012)
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Volume 8 (2011)
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Volume 7 (2010)
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Volume 6 (2009)
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Volume 5 (2008)
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Volume 4 (2007)
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Volume 3 (2006)
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Volume 2 (2005)
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Volume 1 (2004)
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