scholarly journals Green Synthesis of Privileged Benzimidazole Scaffolds Using Active Deep Eutectic Solvent

Molecules ◽  
2019 ◽  
Vol 24 (16) ◽  
pp. 2885 ◽  
Author(s):  
Maria Luisa Di Gioia ◽  
Roberta Cassano ◽  
Paola Costanzo ◽  
Natividad Herrera Cano ◽  
Loredana Maiuolo ◽  
...  
Keyword(s):  
Organic Chemistry ◽  
Pharmaceutical Industry ◽  
Deep Eutectic Solvent ◽  
Reaction Medium ◽  
Building Blocks ◽  
Synthetic Methods ◽  
Benzimidazole Derivatives ◽  
The Face ◽  
Analgesic Activities ◽  
Work Up

The exploitation and use of alternative synthetic methods, in the face of classical procedures that do not conform to the ethics of green chemistry, represent an ever-present problem in the pharmaceutical industry. The procedures for the synthesis of benzimidazoles have become a focus in synthetic organic chemistry, as they are building blocks of strong interest for the development of compounds with pharmacological activity. Various benzimidazole derivatives exhibit important activities such as antimicrobial, antiviral, anti-inflammatory, and analgesic activities, and some of the already synthesized compounds have found very strong applications in medicine praxis. Here we report a selective and sustainable method for the synthesis of 1,2-disubstituted or 2-substituted benzimidazoles, starting from o-phenylenediamine in the presence of different aldehydes. The use of deep eutectic solvent (DES), both as reaction medium and reagent without any external solvent, provides advantages in terms of yields as well as in the work up procedure of the reaction.

scholarly journals Green Synthesis of Privileged Benzimidazole Scaffolds using Active Deep Eutectic Solvent

2019 ◽  
Author(s):  
Maria Luisa Di Gioia ◽  
Roberta Cassano ◽  
Paola Costanzo ◽  
Natividad Herrera Cano ◽  
Loredana Maiuolo ◽  
...  
Keyword(s):  
Organic Chemistry ◽  
Pharmaceutical Industry ◽  
Green Chemistry ◽  
Deep Eutectic Solvent ◽  
Reaction Medium ◽  
Building Blocks ◽  
Synthetic Methods ◽  
Benzimidazole Derivatives ◽  
The Face ◽  
Work Up

The exploitation and use of alternative synthetic methods, in the face of classical procedures that do not conform to the ethics of Green Chemistry, represent an ever present problem in pharmaceutical industry. The procedures for the synthesis of benzimidazoles have become a focus in synthetic organic chemistry, as they are building blocks of strong interest for the development of compounds with pharmacological activity. Various benzimidazole derivatives exhibit important activities such as antimicrobial, antiviral, anti-inflammatory and analgesic and some of the already synthesized compounds have found very strong application in medicine praxis. Here we report a selective and sustainable method for the synthesis of 1,2-disubstituted or 2-substituted benzimidazoles, starting from o-phenylenediamine in the presence of different aldehydes. The use of deep eutectic solvent (DES) both as reaction medium and reagent without any external solvent provides advantages in terms of yields as well as in the work up procedure of the reaction.

scholarly journals Montmorillonite K10: An Efficient Organo- Heterogeneous Catalyst for Synthesis of Benzimidazole Derivatives

2020 ◽  
Author(s):  
Sonia Bonacci ◽  
Giuseppe Iriti ◽  
Stefano Mancuso ◽  
Paolo Novelli ◽  
Rosina Paonessa ◽  
...  
Keyword(s):  
Heterogeneous Catalysis ◽  
Building Blocks ◽  
Synthetic Methods ◽  
Benzimidazole Derivatives ◽  
Free Condition ◽  
Short Reaction Time ◽  
Montmorillonite K10 ◽  
Solvent Free Condition ◽  
The Face ◽  
Work Up

The use of alternative synthetic methods, in the face of traditional processes that do not conform to the principles of Green Chemistry, represent a problem in the pharmaceutical industry. The procedures for the synthesis of benzimidazole derivatives have become a focus in synthetic organic chemistry, as they are building blocks of strong interest for the synthesis of compounds with pharmacological activity. Various benzimidazole derivatives have found very strong application in medicine and their synthesis is reported in the literature. A simple and environmental Montmorillonite K10 (MK10) catalyzed method for the synthesis of benzimidazole derivatives has been developed. The use of MK10 as heterogeneous catalysis provides various advantages in terms of yields, in the work up procedure of the reaction, selectivity and the possible recycle of catalyst without waste formation. The reactions were carried out in solvent free condition and in short reaction time using an inexpensive and environmentally friendly heterogeneous catalysis and it has been shown that the reaction process is applicable in the industrial field.

The importance of synthetic chemistry in the pharmaceutical industry

Science ◽  
2019 ◽  
Vol 363 (6424) ◽  
pp. eaat0805 ◽  
Author(s):  
Kevin R. Campos ◽  
Paul J. Coleman ◽  
Juan C. Alvarez ◽  
Spencer D. Dreher ◽  
Robert M. Garbaccio ◽  
...  
Keyword(s):  
Drug Discovery ◽  
Pharmaceutical Industry ◽  
Synthetic Methods ◽  
Past Century ◽  
Synthetic Chemistry ◽  
Drug Discovery And Development ◽  
The Past ◽  
New Concepts ◽  
The Face ◽  
Chemical Matter

Innovations in synthetic chemistry have enabled the discovery of many breakthrough therapies that have improved human health over the past century. In the face of increasing challenges in the pharmaceutical sector, continued innovation in chemistry is required to drive the discovery of the next wave of medicines. Novel synthetic methods not only unlock access to previously unattainable chemical matter, but also inspire new concepts as to how we design and build chemical matter. We identify some of the most important recent advances in synthetic chemistry as well as opportunities at the interface with partner disciplines that are poised to transform the practice of drug discovery and development.

scholarly journals Experimental investigation on the correlation between the physicochemical properties and catalytic activity of six DESs in Kabachnik-Fields reaction

2020 ◽  
Author(s):  
Shaibuna Machingal ◽  
Sreekumar Krishnapillai
Keyword(s):  
Physicochemical Properties ◽  
Deep Eutectic Solvent ◽  
Reaction Medium ◽  
Deep Eutectic Solvents ◽  
One Pot ◽  
Dimethyl Phosphite ◽  
Type Iv ◽  
Short Period ◽  
Regular Work ◽  
Work Up

Physicochemical properties of six Type IV- Deep eutectic solvents formed from ZrOCl2.8H2O/ CeCl3.7H2O   with urea, ethylene glycol & glycerol were compared. The study was performed by correlating the properties of DESs with their activity in Kabachnik-Fields reaction. Among the six DESs, lower density, viscosity, higher acidity & thermal stability were observed for DES 1(Deep eutectic solvent developed from ZrOCl2.8H2O and urea at 1: 5 ratio) and is reported as an excellent catalyst and reaction medium for the productive synthesis of α-aminophosphonates within a short period of time. One pot reaction of an aldehyde, dimethyl phosphite and amine (Kabachnik-Fields/ Phospha-Mannich reaction) took place at room temperature to give the corresponding α-aminophosphonates in good yield and the precipitation of these products in to water avoided the regular work up process. Catalyst was recycled up to five times without any loss in its activity.

Pyrazole Carboxylic Acid and Derivatives: Synthesis and Biological Applications

2020 ◽  
Vol 17 ◽  
Author(s):  
Adnan Cetin
Keyword(s):  
Organic Chemistry ◽  
Biological Activity ◽  
Carboxylic Acid ◽  
Heterocyclic Compounds ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Building Blocks ◽  
Literature Survey ◽  
Synthetic Methods ◽  
Biological Applications

: The heterocyclic compounds are the building blocks for synthesis of the different biological active compounds in the organic chemistry. Heterocyclic compounds have versatile synthetic applicability and biological activity. Pyrazole carboxylic acid derivatives are significant scaffold structures in heterocyclic compounds due to biologic activities such as antimicrobial, anticancer, inflammatory, antidepressant, antifungal anti-tubercular and antiviral etc. The aim of this mini-review is an overview synthesis of pyrazole carboxylic acid derivatives and their biologic applications. The summarized literature survey presents in detail biological activities of pyrazole carboxylic acid derivatives and their various synthetic methods. This mini-review can be guide to many scientists in medicinal chemistry.

scholarly journals Modern Synthetic Methods for the Stereoselective Construction of 1,3-Dienes

Molecules ◽  
2021 ◽  
Vol 26 (2) ◽  
pp. 249
Author(s):  
Raquel G. Soengas ◽  
Humberto Rodríguez-Solla
Keyword(s):  
Organic Chemistry ◽  
Natural Products ◽  
Functional Group ◽  
Biological Activities ◽  
Synthetic Methods ◽  
Bond Forming ◽  
Drug Candidates ◽  
The Past ◽  
Wide Range

The 1,3-butadiene motif is widely found in many natural products and drug candidates with relevant biological activities. Moreover, dienes are important targets for synthetic chemists, due to their ability to give access to a wide range of functional group transformations, including a broad range of C-C bond-forming processes. Therefore, the stereoselective preparation of dienes have attracted much attention over the past decades, and the search for new synthetic protocols continues unabated. The aim of this review is to give an overview of the diverse methodologies that have emerged in the last decade, with a focus on the synthetic processes that meet the requirements of efficiency and sustainability of modern organic chemistry.

α-Aminoboronates: recent advances in their preparation and synthetic applications

2021 ◽  
Author(s):  
Wenbo Ming ◽  
Harjeet S. Soor ◽  
Xiaocui Liu ◽  
Alina Trofimova ◽  
Andrei K. Yudin ◽  
...  
Keyword(s):  
Building Blocks ◽  
Synthetic Methods ◽  
Mechanistic Explanations ◽  
Recent Advances

This review summarizes new methodology for the synthesis of α-aminoboronates, including asymmetric synthetic methods and mechanistic explanations of reactivity. Applications of α-aminoboronates as versatile synthetic building blocks are also discussed.

Modern trends in the development of organic chemistry

2021 ◽  
pp. 71-78
Author(s):  
Irina Anatolievna Selivanova ◽  
Roman Petrovich Terekhov ◽  
Amir Khalilovich Taldaev
Keyword(s):  
Organic Chemistry ◽  
Pharmaceutical Industry ◽  
Scientific Research ◽  
Modern World ◽  
International Conference ◽  
Qualified Personnel ◽  
Scientific Potential ◽  
Young Researchers

The role of organic chemistry and other chemical disciplines in the system of training qualified personnel for the pharmaceutical industry is indisputable. In what direction is chemistry developing in the modern world? What innovative directions does chemistry offer to drug developers? Can a robot synthesize a new compound? How to achieve practically significant results of scientific research? How may the obtained results be published in highly rated journals? These and many other topics were widely discussed at the XII International Conference of Students and Young Scientists in Chemistry «Mendeleev-2021» held in the fall of 2021. This article is published to attract young researchers’ attention to topical issues at the interface of chemistry and pharmacy and assist them in realizing their creative scientific potential.

scholarly journals Cellulose recycling as a source of raw chirality

2013 ◽  
Vol 85 (8) ◽  
pp. 1683-1692 ◽  
Author(s):  
Valeria Corne ◽  
María Celeste Botta ◽  
Enrique D. V. Giordano ◽  
Germán F. Giri ◽  
David F. Llompart ◽  
...  
Keyword(s):  
Organic Chemistry ◽  
Organic Carbon ◽  
Asymmetric Synthesis ◽  
Building Blocks ◽  
Biologically Active ◽  
Raw Material ◽  
Chiral Auxiliaries ◽  
High Chemical ◽  
Chiral Structure

Modern organic chemistry requires easily obtainable chiral building blocks that show high chemical versatility for their application in the synthesis of enantiopure compounds. Biomass has been demonstrated to be a widely available raw material that represents the only abundant source of renewable organic carbon. Through the pyrolitic conversion of cellulose or cellulose-containing materials it is possible to produce levoglucosenone, a highly functionalized chiral structure. This compound has been innovatively used as a template for the synthesis of key intermediates of biologically active products and for the preparation of chiral auxiliaries, catalysts, and organocatalysts for their application in asymmetric synthesis.

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