Current Organic Synthesis - Current Issue

Palladium-catalyzed carbonylative cross-coupling reactions with various carbon monoxide (CO) sources cultivate competent routes for the synthesis of bulk and value-added chemicals. However, the practical use of this odorless, inflammable, lethal gas has always raised a concern for chemists. The attention and advancement of various CO-surrogates is surely welcomed as a green alternative to CO-gas. However, the main concern lies in the suitability and scalability of these CO-surrogate-driven reactions. Literature showed the progress of various ways to make in-situ CO from these CO surrogates. One of the most convenient sources is using metal carbonyls which are already known to lose CO easily. Among all the kinds, Mo(CO)6 gained much popularity but its toxic nature and demand for high temperatures restricted its use. However, Co2(CO)8 is popular as a catalyst but as an in-situ CO-source reports are scarce. This low-melting CO-releaser was found effective in flourishing aminocarbonylation, alkoxycarbonylation, and reductive carbonylation under mild conditions. This mini-review portrays the recent developments of palladium-catalyzed carbonylation reactions using Co2(CO)8 as a CO source.

Unsaturated pyrazolones can participate in organocatalytic reactions with various substrates to form spiro-cyclic pyrazolones, and fuzed-pyrazolone heterocycles. The present review describes progress since 2013 in the organocatalysis transformations of unsaturated pyrazolones. Pyrazolones are prevalent structural motifs in a wide variety of natural products and drug or drug-like molecules. A series of nitrogen-containing pyrazolones exhibits anticancer, antimicrobial, anti-inflammatory, anticonvulsant, antidepressant, antidiabetic, and antipyretic activities. Especially, chiral spiro-cyclic pyrazolones are recognized as targets in natural products and clinical pharmaceuticals. Organocatalytic systems are powerful and reliable approaches that allow us to build structurally complex molecules in an enantioselectively and diastereoselectively manner. Avoiding the use of transition metal catalysts, readily available bifunctional organocatalysts, and the performance of the reaction at ambient temperature are other advantages of these catalytic systems. Despite considerable progress in this field, it is still one of the challenging goals for chemists to make new biologically active heterocyclic molecules.

The biopolymer chitosan, which is derived from chitin, has shown great promise for tissue regeneration and regulated drug delivery. Its broad-spectrum antibacterial action, low toxicity, biocompatibility, and many other attributes make it appealing for use in biomedical applications. Crucially, chitosan may be synthesized into a range of forms that can be customized to provide desired results, such as hydrogels, membranes, scaffolds, and nanoparticles. Hydrogels that are biocompatible and self-healing are innovative soft materials with considerable potential for use in biomedical applications. Hydrogels that self-heal using chitosan, which are mostly made by dynamic imine linkages, have gained a lot of interest because of their great biocompatibility, moderate preparation requirements, and capacity to mend themselves in a physiological setting. In this study, a summary of the applications of chitosan-based self-healing hydrogels in bone, cartilage, and tooth tissue regeneration and drug delivery is provided. Lastly, we have mentioned the difficulties and potential outcomes for the biomedical field's creation of hydrogels based on chitosan that can mend themselves.

The current review aimed to provide an understanding of the preparation, reactions, and biological action of thiazoles. The purpose of this review was to focus on the progress made in the synthesis of physiologically effective thiazole products with their interactions. A combinatorial approach was proposed, and extensive attempts were made in the search for thiazoles by chemists in many domains due to the information of multiple artificial pathways and variable physics-chemical factors of thiazoles. In this regard, the biological activities linked to thiazole and the processes used in its production were thoroughly discussed in this study. The research period covered in this review was from 1905 to 2024, providing a useful and convenient strategy for the synthesis of numerous thiazole derivatives. Moreover, research on such reactions is still ongoing and undoubtedly will provide new fused functionalized compounds of both industrial and biological interests. A literature survey revealed that a great deal of interest has been focused on the synthesis and reaction of thiazoles due to their wide range of biological activities. Remarkable insights into different synthetic paths and modified physical-chemical features of such thiazoles would be helpful for chemists worldwide.

Bitter melon (Momordica charantia L.) is a member of the Cucurbitaceae, which is also known as bitter squash, bitter gourd, karela, Goya melon and balsam pear. It is a rich source of different vitamins, potassium, zinc and other nutrients.

The main pharmaceutical benefits of bitter melon are “antiinflammatory”, “antioxidant activity”, “antimicrobial characteristic”, “anticancer activity”, and “antihelmintic activity”, “antidiabetic effects”, “antiinflammation activity” and “treat skin conditions”. Its fruit is the main part of the plant which has been used for medicinal and food purposes.

The primary metabolites in bitter gourd are common sugars, chlorophyll and proteins while secondary metabolites are carotenoids, alkaloids, phenolics, curcubitane triterpenoids, saponins, etc.

The present review aims to study and survey on the nearly up-to-date results and findings regarding the pharmaceutical advantages and health benefits of bitter melon in an organic life.

Derivatives of pyrimidinone, dihydropyrimidinone, and 2,4-diaryl-substituted pyrimidines were synthesized by cyclocondensation of α-aminoamidines with various saturated carbonyl derivatives and their analogs. The therapeutic potential of the newly synthesized derivatives for cancer treatment was evaluated using molecular docking calculations. The molecular docking results indicate that some of the synthesized diaryl derivatives of pyrimidine exhibit high binding affinity towards PIK3γ.