A Highly Stereoselective Chiral Auxiliary‐assisted Reductive Cyclization to Furoindoline

Chemistry & Biodiversity

2022

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Cancer is still one of the leading causes of death worldwide. Many researchers are working to design and develop heterocyclic-based drugs with the potential to treat cancer at various stages. There is always an unmet need to discover new anticancer drugs to treat different types of cancer. Based on literature reports, it was evident that hybrid 1,2,4-triazoles exhibit a wide spectrum of biological potential (particularly potent anticancer activity), as compared to the corresponding monocyclic compounds. In this review, we summarized fused/hybrid 1,2,4-triazole and poly-functionalized 1,2,4-triazoles as anticancer agents. Triazole may be fused with other heterocyclic scaffolds like pyrimidine, pyridine, piperidine, quinoxaline, quinazoline, thiadiazine, indole, phthalazine etc. A clear explanation of the method of synthesis, structure-activity relationship, and in vitro results plus the inhibitory concentration of new molecules are focused on in this review article.

Section: Discussionmentioning

confidence: 99%

Synthetic and Medicinal Perspective of 1,2,4‐Triazole as Anticancer Agents

Rathod

Chemistry & Biodiversity

2022

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Microwave‐assisted diversified synthesis of pyrimidines: An overview

Journal of Heterocyclic Chem

2021

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Pyrimidines and their hybrid molecules have continued to be a favorable area for organic chemists owing to their richness in natural and synthetic compounds with multifarious involvement in pharmaceuticals and polymers and act as ligands. Different novel and greener synthetic protocols were developed in the last decades, but microwave‐assisted synthetic protocols played a significant role in constructing pyrimidine and its derivatives. In this article, we summarized the microwave‐supported strategy for the construction of pyrimidine fused or linked/tethered with other heterocycles, polysubstituted pyrimidines, solid‐supported synthesis of pyrimidines, and ionic liquid‐catalyzed strategies for the synthesis of pyrimidine and its derivatives reported in the last decade. Solid‐supported protocols using resins and ionic liquid‐catalyzed strategies afforded the corresponding products with excellent yield by dual activation. In most of the reports, the microwave‐irradiated approach was compared with conventional/traditional heating and found better in terms of reaction time, yield, atom economy, adherence with green chemistry principles, and reduction in purification wastage. Various authors evaluated the in vitro potential of synthesized pyrimidine derivatives for antimicrobial and antimalarial potential, and found moderate to excellent biological activity.

CuI/DBU‐Mediated MBH Reaction of Isatins: A Convenient Synthesis of 3‐Substituted‐3‐hydroxy‐2‐oxindole

Rawal

2020

ChemistrySelect

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An efficient, simple and economic Morita‐Baylis‐Hillman approach for construction of 3‐hydroxy‐3‐substituted‐2‐oxindole was proceeded smoothly from isatin derivatives and methyl acrylate/acrylonitrile using mild catalytic conditions. It was demonstrated that proper selection of catalyst and reaction medium would differentiate the feasibility of reaction and yield of the final product. Reaction condition was explored the novel combination of Copper Iodide (CuI) and 1,8‐Diazabicyclo [5.4.0] undec‐7‐ene (DBU) in the presence of dichloromethane (DCM) as the medium. This strategy provides a facile access to various derivatives with good to excellent yields in short span of time. The resulting derivatives can serve as a valuable synthetic building block for pharmaceuticals and natural products.