Current Organic Synthesis - Volume 21, Issue 2, 2024

Julia-Lythgoe olefination (or simply Julia olefination) is an olefination process between phenyl sulfones and aldehydes (or ketones) to give alkenes after alcohol functionalization and reductive elimination using sodium amalgam or SmI2. It is mainly used to synthesize E-alkenes and is a key step in numerous total syntheses of many natural products. This review exclusively deals with the Julia-Lythgoe olefination and concentrates mainly on the applications of this reaction in natural product synthesis covering literature up to 2021.

“The founder of green chemistry explains how chemicals manufacturing must change to support a sustainable future.” In this review, Green chemistry is considered in the synthesis of heterocycles compounds containing Pyrimidine nuclei using different catalyzes, solvents, and techniques for the synthesis of pyrimidine derivatives that achieve sustainability. The mentioned fused heterocycles are classified according to the type of ring system. The yield of the target molecules reported in the review is given in the reaction's last step.

Background: Isocyanide is an intriguing one-carbon synthon that is frequently employed in a variety of carbon-carbon and carbon-heteroatom bond-forming reactions. Isocyanide-based multicomponent reactions (IMCRs) are effective synthetic tools in organic synthesis for the preparation of complex heterocyclic molecules. The IMCRs in water have become an attractive research direction, enabling simultaneous growth of both IMCRs and green solvents towards ideal organic synthesis. Objective: The goal of this review is to provide a general overview of IMCRs in water or biphasic aqueous systems for accessing various organic molecules, as well as an examination of their benefits and mechanistic insights. Conclusion: High atom economies, mild reaction conditions, high yields, and catalyst-free processes are crucial features of these IMCRs in water or biphasic aqueous systems.

Click Chemistry, as a powerful tool, has been used for the synthesis of a variety of 1,2,3-triazoles. Among click cycloaddition reactions, intramolecular click reactions carried out in azido-alkyne precursors has not been thoroughly reviewed. Hence, in this review, we have summarized and categorised the recent literature (from 2012 on) based on the azidoalkynyl precursor's type and a brief and concise description of the involved mechanisms is presented. Accordingly, we have classified the relevant literature into three categories: (1) substitution precursors (2) addition and (3) multi-component reaction (MCR) products.

Introduction: A simple method for the preparation of 5-(trifluoroacetyl)imidazoles was elaborated. Methods: The reaction of trifluoromethyl(α-bromoalkenyl)ketones with benzimidamides was employed to afford the target heterocycles in good yields. Results: The assembly of imidazole core proceeds viaaza-Michael adduct formation followed by intramolecular nucleophilic substitution and spontaneous aromatization as an oxidation sequence. Conclusion: The yields of target imidazoles can be improved by the use of soft oxidizing agents.

Objective: In this study, a simple triethylammonium salt of phosphoric acid (triethylammonium dihydrogen phosphate) (4) in the liquid state was utilized as an inexpensive, efficient one-pot three components, solvent-free synthesis of thiazolidine-4-one derivatives, with good to excellent yields. Techniques such as FT-IR, ¹H-NMR, ¹³C-NMR, ¹³C-NMR-DEPT-135, and MS. were used for the structural elucidation. The high biotic efficiency of the newly obtained compounds was confirmed by in vitroantimicrobial action against Gram-positive (S. Aureus), Gram-negative bacteria (P. Aeruginosa and E. Coli) and antifungal activity (C. Albicans) viamicroplate titer dilution technique. Finally, a molecular docking study was performed with a resolved crystal structure of S. AureusD-alanine alanyl carrier protein ligase (PDB ID: 7VHV). This investigation aimed to synthesize a new series of thiazolidine-4-one derivatives combined with benzoxazole moiety. Material and Methods: Ionic liquid assistance one-pot solvent-free synthesis method used to synthesize a new series of thiazolidine-4-one derivative 10(a-e). Results: Structural identification of new synthesis and biological evaluation viatechniques of (IR, ¹H-NMR, ¹³C-NMR, ¹³C-NMR-DEPT-135, and MS). Conclusion: Ionic liquid is utilized as an inexpensive, efficient one-pot three-component solvent-free synthesis of thiazolidine-4-one derivatives with good to excellent yields. Most of the synthesized compounds showed high biological and anti-fungal activity, in line with the docking study against mentioned microorganism and crystal structure of PDB (ID: 7VHV), respectively.