Letters in Organic Chemistry - Volume 21, Issue 9, 2024

2-Hydroxymethyl piperazine is a crucial structural unit and essential intermediate in the drug development process. However, there are few reported methods for synthesizing 2- hydroxymethyl piperazine substituted at position 5. Herein, the 2-hydroxymethyl piperazines are synthesized from serine methyl ester hydrochloride and N-Boc-L-amino acids through a four-step reaction of condensation, deprotection, cyclisation, and reduction. This synthetic route has several advantages, including mild reaction conditions, availability of reagents, non-racemic composition, and the potential for gram-scale synthesis. In this study, we present a mild and effective synthetic method for preparing para-substituted 2-hydroxymethyl piperazine.

A series of novel activated esters of morphine were synthesized as alternatives to the triflate ester and submitted to hydrogenolysis conditions. Of these, only the novel nonaflate ester could be transformed with full conversion into the useful intermediate, 3-deoxymorphine, which was isolated in good yield and high purity without chromatography. This conversion proceeded significantly faster than for the triflate ester and with synthesis of the intermediate nonaflate at much reduced cost, an important factor for the large-scale preparation of 3-deoxymorphine in drug development projects.

In this paper, we have reported solvent solvent-free method for Knoevenagel condensation reaction of various aldehydes with active methylene compounds using thiourea and ammonium chloride. The developed method demonstrated high efficiency in the formation of C-C bond. The reaction proceeds smoothly under mild and solvent-free conditions and the products obtained are in excellent yield in very short duration. This method is applicable to a wide range of aldehydes with active methylene compounds.

Quinoline is one of the promising and prominent biologically active N-based heterocyclic compounds. This review paper aims to discuss the synthetic approaches, summarized from various research articles on the preparation of quinoline derivatives intended for different therapeutic activities like antifungal activity, anticancer activity, anticonvulsant activity, antitubercular activity, antimalarial activity, anti-Alzheimer activity and so on. The comprehensive study complies with all related publications and trademark publications demonstrating the synthesis and biological aspects of quinoline derivatives. Various types of quinoline hybrids were synthesized and treated for therapeutic activity, including anticancer, antitubercular, anti-Alzheimer, antioxidant, and antifungal activity, which have been analyzed. Quinoline is a planner hetero-aromatic compound with the chemical formula C9H7N. Several wellknown synthetic routes to the quinoline skeleton include Friedlander synthesis, Knorr quinoline synthesis, and Skraup reaction. Researchers may use other techniques or alter current strategies to reach their objectives, depending on what exact structure and therapeutic action they are investigating. The availability of starting materials, reaction conditions, scalability, desired regioselectivity, and functionalization of the quinoline core all have a role in the choice of synthetic method. This review covers the latest literature and knowledge on the synthetic procedures for numerous quinoline and its derivatives and their biological and pharmacological application.

In this study, an efficient method for the synthesis of one type of aromatic ether was introduced, and its antitumor activity was investigated. Specifically, (diacetoxyiodo)arene was prepared from 2-methyliodobenzene and used to oxidize the 4-nitrophenol to give the aromatic ether. Our study further found that aromatic ether has a strong apoptotic effect on U937 monocytes, suggesting that it might be developed as a new drug for the treatment of acute myeloid leukemia.

Introduction: In this investigation, we employed a continuous flow reactor to synthesize nickel (Ni) nanoparticles exhibiting uniform size distribution and excellent stability. Our focus centered on exploring the impact of reactant dilution and flow rate on the synthesis process. Result: It was observed that the optimization of these parameters played a pivotal role in obtaining small-sized Ni nanoparticles. Specifically, we achieved successful synthesis using a solution of 0.00025 M NiCl2·6H2O and 0.002 M NaBH4, with a flow rate of 25 mL/h. The resulting Ni nanoparticles were effectively coated with the CTAB surfactant, as confirmed through thorough analysis using TEM and PSD techniques. Additionally, the interaction between the surfactant and nanoparticles was verified via FTIR analysis. We subjected them to high-pressure alkene hydrogenation to assess the catalytic activity of the synthesized Ni nanoparticles. Method: Encouragingly, the Ni nanoparticles exhibited excellent performance, producing hydrogenated products with high yields. Moreover, we capitalized on Ni nanoparticles' catalytic effect for synthesizing two natural compounds, brittonin A and dehydrobrittonin A. Remarkably, both compounds were successfully isolated in quantifiable yields. This synthesis protocol boasted several advantages, including low catalyst loading, omission of additives, broad substrate scope, straightforward product separation, and the ability to recover the catalyst up to eight times. In summary, this study effectively showcased the potential of continuous flow reactor technology in synthesizing stable and uniformly distributed nanoparticles. Conclusion: Additionally, it highlighted the effectiveness of Ni nanoparticles as catalysts in various chemical reactions. The findings from this study hold significant implications for developing more efficient and sustainable chemical synthesis protocols.

The development of density functional theory has led to the consideration of computational chemistry in the design and development of interactions of new drugs in the gas phase with nanocarriers. In the present study, the interaction of ibuprofen with alginic acid (as a nanocarrier) has been investigated using density functional theory (DFT) in the gas phase (M06-2X/6-31+G*). A study on the effects of ibuprofen's interaction with the compounds present in alginic acid has been conducted, focusing on the electronic properties, the chemical shift tensors, and the natural bond orbital. Based on the results of UV spectra, the compound 6-thioguanine has been found to be changed into an alginic acid/ibuprofen complex. The quantum theory of atoms in molecules showed the interaction of ibuprofen to be mainly driven by non-covalent bonds with alginic acid during complex formation. A hydrogen bond has been found to be formed between the oxygen atoms of alginic acid and ibuprofen's hydrogen atoms. Consequently, alginic acid has been used for delivering ibuprofen to diseased cells.