Current Organic Synthesis - Volume 14, Issue 4, 2017

Chiral ionic liquids (CILs) have potential application in asymmetric organic synthesis, chiral drug synthesis, stationary phases in chiral chromatography, optical resolution of racemic mixtures and chiral shifting reagents in NMR spectroscopy. CILs may possess central, planar or axial chirality and can be synthesized from chiral pool or via asymmetric synthesis. Although, the synthesis of these species is difficult and cos Read More

The diversity and chemoselectivity in rearrangements of N,N’-diarylhydrazines are reviewed and summarized. The symmetric N,N’-diarylhydrazines without any para-substituents generally favor para-benzidine rearrangement accompanying diphenyline rearrangement, even semidine rearrangement in some cases, while those with single or double N-naphthyl(s) or double para-substituent phenyls undergo ortho-benzidi Read More

In recent decades, a large number of reports related to synthesis of N, O and S containing heterocycles have appeared owing to a wide variety of their biological activity. We need a catalyst system that not only shows high activity and selectivity but also possesses the ease of catalyst separation and recovery. Therefore, the different metals are used as a catalyst for the synthesis of oxygen containing heterocyclic comp Read More

The development of efficient routes to pyrazines and their ring fused analogues is an attractive area of research since these compounds are now widely recognized as important N-heterocycles for their potential use in medicinal and agricultural scientific fields. In this review, we describe the most representative and interesting methods for the synthesis of pyrazines from N-propargylamines. Mechanistic aspects of the reactio Read More

Michael addition reaction has been a very classical reaction in the field of organic synthesis. It is widely used to synthesize all kinds of natural products and drugs. Since the beginning of 21st century, people's environmental awareness has been enhanced and the research on green chemistry has been advanced. The Michael addition method with high efficiency, simplicity and greenness has been the goal pursued by Read More

Background: The chemistry of tetrazine has gained an increased attention in the last decades due to their applications materials science and coordination chemistry. 1,3-Dipolar cycloaddition of nitrile imines to C60 is the standard method for annelating the pyrazoline ring to the fullerene sphere. The interest in the chemistry of hydrazonoyl halides is a consequence of the fact that they undergo a wide variety of reactions, Read More

Background: As evidence suggests a key role played by the low-activity pyruvate kinase M2 (PKM2) in tumor progression it emerges as an attractive target in cancer therapy. Objective: The aim of the present study was to design and develop a synthetic method for the preparation of a new sulfonamide compound as a potential PKM2 activator. Method: A seven-step synthesis procedure was carried out. It started with tert-but Read More

Background: 2-Substituted benzothiazoles are a class of heterocyclic compounds that have a wide range of applications in agriculture, pharmaceutical and chemical industry due to their wide spectrum of biological and biophysical properties. Benzothiazole is usually prepared by the condensation of 2-aminobenzenethiols or 2,2'-disulfanediyldianilines, the cyclization of thioformanilides, or the sulfurization of 2-haloanili Read More

Background: β-Lactam antibiotics are plenty applied for the treatment of bacterial infections.Other biological activities and utilizing as a building block of 2-azetidinones is also well reported. The most useful method for the synthesis of 2-azetidinones is the Staudinger reaction. Generally ketenes were prepared from acyl halides which acyl halides shows unfavorable results such as low stability, low yield of products, and dif Read More

Background: The production of 5-hydroxymethylfurfural (5-HMF) from biomass provides an alternative pathway for many commercial chemicals and polymers particularly for countries with high insolation such as sub-Saharan Africa. Objective: The goal is continuous or semi-continuous dehydration of glucose and fructose to 5-HMF over a reusable castalyst in a process which is commmercial viable. Method: We deploy a Read More

Background: One-pot reactions have gained considerable and wide range of interests in the field of chemistry due to their simplicity and economy. Comparing to the step-by-step reactions that involve the formation of individual bonds for a given target product, the greatest attribute of one-pot reactions, is the formation of several bonds in one-pot operation without intermediate isolation, reaction condition changing and further Read More

Background: In the recent years the 2-imino-1,3-thiazine and 2-iminothiazolidine ring systems can be found as moieties in biologically relevant compounds, including BACE1 inhibitors, or cannabinoid receptor agonists, while monoterpene-based 2-imino-1,3-thiazines, prepared from chiral 1,3-amino alcohols exhibiting pronounced antiproliferative activity. Methods: The antiproliferative activities of the prepared compounds Read More

Background: Thiazole ring is one of the most important heterocyclic ring systems due to their wide range of biological activities. Objective: we became interested in synthesizing a new series of thiazole derivatives to investigate their antitumor activity against liver and colon cancer cell lines. Method: A novel series of 5-arylazothiazoles was prepared from 2-(-1-morpholino-1-(2-arylhydrazono)propan-2- ylidene)-hydrazinecarbo Read More