Current Organic Synthesis - Volume 19, Issue 5, 2022

Background: Betti bases are pharmaceutically and synthetically important scaffolds due to their diverse range of biological activities and applications in key synthetic transformations in organic synthesis. Objective: This work has been sought to contribute to the development, design, and implementation of an improved green methodology with higher atom economy and lower E-factor values for the synthesis of Betti Read More

Background: 1,2,4-triazoles scaffolds display significant biological activities due to hydrogen bonding, solubility, dipole character, and rigidity. Objective: The core motif of 1,2,4-triazoles plays a vital role in clinical drugs such as Rizatriptan (antimigraine), Ribavirin (antiviral), anastrozole (anticancer), etizolam (anxiolytic), estazolam (anticonvulsant), alprazolam (anti-hypnotic), letrozole (aromatase inhibitor), loreclezole (an Read More

Background: SKLB1039 is a potent, highly selective, and orally bioavailable EZH2 inhibitor, which significantly inhibited breast tumor growth and metastasis in pre-clinical studies. In a previously reported synthesis of SKLB1039, the yields of several steps were low, which led to an overall yield of less than 10%. In addition, flash chromatography was required for the purification of several intermediates using this route. Objective Read More

Background: Arylidenemalononitriles are valuable synthons for the construction of a variety of novel complex heterocyclic motifs, fused heterocycle derivatives, and spirocyclic compounds. They are versatile chemical intermediates and have increasing applications in industry, agriculture, medicine, and biological science. Objective: The aim of this review is to highlight the preparation methods and reactions of a Read More

2,3-Diaminomaleonitrile (DAMN), a tetramer of hydrogen cyanide, displays weakly basic properties and has reactivity comparable to o-phenylenediamine. It has emerged as a versatile, cheap as well as a readily accessible building block towards the synthesis of a variety of organic compounds. The present review focuses on the applications of 2,3-diaminomaleonitrile for the synthesis of Schiff’s base, imidazoles, pyr Read More

Chalcone-derived isoxazole scaffolds remain the central focus due to their greater biological, clinical, and pharmacological properties. The present study reviews the synthesis of various chalcone derived - 5- membered isoxazoline and isoxazole scaffolds with the available literature until 2021.

Aims and Objective: Condensation of 5-hetarylidene-2,2-dimethyl-1,3-dioxane-4,6- diones with 5,5-dimethyl-3-arylamino-2-cyclohexanones yields 1-aryl-4-hetaryl-7,7-dimethyl-2,5- dioxo-l,2,3,4,5,5,7,8-octahydro-quinolines. The structures of all the synthesized compounds have been verified by IR, 1H-NMR, 13C-NMR, and mass spectral methods. The 13C-NMR assignments were supported by HSQC and HMBC experiments. Moreo Read More

Background: In today’s world, rising temperature due to global warming is caused by higher concentration of carbon dioxide (CO2) emissions in the atmosphere. Metal-Organic Framework (MOF) materials have the potential to be used in carbon dioxide capture and utilization technology. Objective: The purpose of this work is to prepare metal-organic framework materials by a benign synthesis method using water as the s Read More