In terms of pharmaceuticals and biological applications, synthesis of complex organic molecules is a significant and fast‐developing area. In this context, organic electrosynthesis is an alternative way to the traditional methods for chemo‐, regio‐, and stereoselective syntheses. Electro‐organic reactions occur at room temperature and normal pressure, through transferring electrons. It has been found that electrosynthesis is a mild approach for preparing electrophilic substrates, bases, and nucleophiles in situ, from highly stable and low‐level reagents; which can be further applied to make heterocycles more accessible. While several promising methods exist, multi‐component reactions (MCRs) have drawn much attention both in academia and industry worldwide, since they are cost‐efficient and environmentally friendly. Combining the electrosynthesis and MCRs has produced a great strategy in the field of organic synthesis for industry and research. This review focuses on recent advances in the electrochemical synthesis of heterocyclic compounds via multi‐component reactions, reported between 2015 and March 2023.
31 October 2024 in Journal of the American Chemical Society
Although radioactive experiments are necessary in radiopharmaceutical drug discovery and theranostic cancer research, they are expensive, require special facilities, and face certain restrictions. Thus, finding techniques not involving radioactivity is highly beneficial for minimizing these disadvantages in such research. In this regard, methods using inductively coupled plasma-mass spectrometry (ICP-MS) have emerged as viable alternatives to traditional radioactive approaches. Despite its potential, practical applications of ICP-MS in radiopharmaceutical cancer research have only emerged in recent years. This Perspective focuses on the development and implementation of nonradioactive ICP-MS-based assays in radiopharmaceutical research and aims to inspire future research efforts in this area.
The unique reactivity and beneficial features of the 5-aminotetrazole synthon (1H-tetrazol-5-amine) have made it a versatile and effective building block in the synthesis of heterocyclic compounds. In addition, several drugs containing this scaffold with a wide array of biological properties have been already introduced. Heterocyclic structures are the backbone of many biologically active and industrially important compounds. 5-Aminotetrazole is one of the favored synthons used in the preparation of heterocycle-bearing compounds, especially in multicomponent synthesis. This review highlights a comprehensive overview of the emerging applications of 5-aminotetrazole as a key component in the synthesis of heterocyclic frameworks through multicomponent reactions, reported between 2017 and July 2023.1 Introduction2 5-Aminotetrazole3 Tetrazolopyrimidine Compounds4 Spiro Compounds5 Miscellaneous6 Conclusion
25 January 2021 in Organic & Biomolecular Chemistry
In radiopharmaceutical syntheses, maleimide is commonly used for linking thiol-bearing bioactive molecules to metal–complexing ligands (chelators). However, due to instability of the resulting linkage, phenyloxadiazolyl methylsulfone (PODS) was developed as an alternative to maleimide. This coupling strategy has never been attempted with HBED which is a powerful chelator for gallium-radiolabeling especially at ambient temperature. Here we present HBED-CC-PODS as a bifunctional chelator scaffold for the site-selective conjugation of thiol-bearing vectors and [68Ga]Ga-radiolabeling.