General and Synthetic Methods

Anthracene derivatives have been used for a wide range of applications and many different synthetic methods for their preparation have been developed. However, despite continued synthetic efforts, introducing substituents in some positions has remained difficult. Here we present a method for the synthesis of 2,3,6,7-substituted anthracene derivatives, one of the most challenging anthracene substitution patterns to obtain. The method is exemplified by the preparation of 2,3,6,7-anthracenetetracarbonitrile and employs a newly developed, stable protected 1,2,4,5-benzenetetracarbaldehyde as the precursor. The precursor can be obtained in two scalable synthetic steps from 2,5-dibromoterephthalaldehyde and is converted into the anthracene derivative by a double intermolecular Wittig reaction under very mild conditions followed by a deprotection and intramolecular double ring-closing condensation reaction. Further modification of the precursor is expected to enable the introduction of additional substituents in other positions and may even enable the synthesis of fully substituted anthracene derivatives by the presented approach.<br>

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Сatalytic Phosphorylation of Aromatic C-H Bonds: from Traditional Approaches to Electrochemistry

Current Organic Chemistry ◽

10.2174/1385272822666191007145336 ◽

2019 ◽

Vol 23 (16) ◽

pp. 1756-1770

Author(s):

Sofia Strekalova ◽

Mikhail Khrizanforov ◽

Oleg Sinyashin ◽

Yulia Budnikova

Keyword(s):

Organophosphorus Compounds ◽

Normal Pressure ◽

Acid Group ◽

Synthetic Methods ◽

Heteroaromatic Compounds ◽

Anti Cancer ◽

Phosphonic Acid Group ◽

Traditional Approaches ◽

Anti Hiv Agents ◽

Anti Hiv

The interest in organophosphorus compounds with a C-P bond is due to their wide use in various fields, especially in medicine and agrochemistry. Prominent examples of anti-cancer, antibacterial, and anti-HIV agents are therapeutic candidates containing a phosphonic acid group fragment. This review provides modern synthetic methods for obtaining phosphorylated aromatic and heteroaromatic compounds with the participation of complexes and salts of various metals developed in recent years as well modern protocol - electrochemical synthesis which allows carrying out reactions at room temperature and normal pressure with no additional oxidants or bases. Herein, we demonstrate new trends and evolution of phosphorylation reactions in catalysis.

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Recent Developments on Synthesis of Indole Derivatives Through Green Approaches and Their Pharmaceutical Applications

Current Organic Chemistry ◽

10.2174/1385272824999201111203812 ◽

2020 ◽

Vol 24 (22) ◽

pp. 2665-2693

Author(s):

Dipayan Mondal ◽

Pankaj Lal Kalar ◽

Shivam Kori ◽

Shovanlal Gayen ◽

Kalpataru Das

Keyword(s):

Biological Activities ◽

Synthetic Methods ◽

Pharmaceutical Chemistry ◽

Indole Derivatives ◽

Biological Studies ◽

Recent Developments ◽

Pharmaceutical Industries ◽

Green Methodology ◽

Conventional Methods ◽

High Yields

Indole moiety is often found in different classes of pharmaceutically active molecules having various biological activities including anticancer, anti-viral, anti-psychotic, antihypertensive, anti-migraine, anti-arthritis and analgesic activities. Due to enormous applications of indole derivatives in pharmaceutical chemistry, a number of conventional synthetic methods as well as green methodology have been developed for their synthesis. Green methodology has many advantages including high yields, short reaction time, and inexpensive reagents, highly efficient and environmentally benign over conventional methods. Currently, the researchers in academia as well as in pharmaceutical industries have been developing various methods for the chemical synthesis of indole based compounds via green approaches to overcome the drawbacks of conventional methods. This review reflects the last ten years developments of the various greener methods for the synthesis of indole derivatives by using microwave, ionic liquids, water, ultrasound, nanocatalyst, green catalyst, multicomponent reaction and solvent-free reactions etc. (please see the scheme below). Furthermore, the applications of green chemistry towards developments of indole containing pharmaceuticals and their biological studies have been represented in this review.

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