Letters in Organic Chemistry - Volume 15, Issue 4, 2018

Background: Biginelli reaction is one of the most important multiple-component chemical reactions which creates 3,4-dihydropyrimidin-2(1H)-ones. Even though Biginelli reaction was reported over a century using different substrates, literature lacks the example of the use of alcohols as a substrate. The substitution of aldehyde component with another functional group has not been explored so far. Method: In the present s Read More

A simple, convenient and facile approach for the synthesis of a series of 2,3- dihydroquinazolin-4(1H)-ones in an environmentally benign method has been developed. This method involves a direct cyclocondensation of 2-aminobenzamide with aromatic aldehydes and ketones using aspartic acid as a catalyst in water.

Introduction: Phenol or carbolic acid is an aromatic compound and has mild acidic nature. In 1834, it was firstly achieved by Friedlieb Ferdinand by the destructive extraction of coal tar. It is used as a significant raw material in quite a lot of chemical manufacturing. Phenol derivatives have been found to possess Antimicrobial, Analgesic, Anti-inflammatory, Antioxidant, Anti-convulsant, Anti-cancer, Anesthetic, Antiseptic and Disinf Read More

Background: The 3-Substituted indoles are found to possess a wide range of biological and pharmacological activities. The efficient and impurity free scalable preparation of 2-(1H-Indol-5-yl)- ethanesulfonic acid methylamide has been successfully achieved for the synthesis of Naratriptan and its novel 3-substituted derivatives. Method: The preparation of 2-(1H-Indol-5-yl)-ethanesulfonic acid methylamide involves the condensat Read More

Background: Chronic myelogenous leukemia (CML) is a myeloproliferative neoplasm that can occur in any age group but often seen in adults and contributing for about 20% of adult leukemias and it may contribute up to 15% of all types of leukemias threatening the globe. Therefore, treatment of CML remains as a major challenge in cancer therapeutics. Methods: We synthesized a library of novel 2-amino-4-(4-substit Read More

Background: In spite of significant progress made toward the synthesis of triazole amino acids as structural scaffolds of peptides and leading structures of new drugs, a need still exists for effective methods of trisubstituted triazole amino acid synthesis. Methods: A protocol based on ruthenium(II)-catalyzed alkyne-azide cycloaddition (RuAAC) was developed to synthesize 5-bromo-1,4,5-trisubstituted 1,2,3-triazole-base Read More

Background: Benzimidazole and benzothiazole subunits exist in many biologically active molecules, natural products, and synthetic compounds. These compounds have recently gained widespread interest due to their key role in medically important compounds, such as those exhibiting anticancer activity, antimicrobial activity, inhibition of hepatitis C virus NS5B polymerase, p38 kinase inhibitory activity, and anti-inflamm Read More

Background: Bis(indolyl)methane derivatives exhibit varied biological and pharmacological properties like antibacterial and antiangiogenic activities, acting as cytotoxic agents and tumor growth inhibitors. Several approaches of bis(indolyl)methane synthesis have been reported, most of them involving condensation of indoles with aldehydes or ketones in the presence of protic or Lewis acids. Also other catalysts like enzymes w Read More

Background: 2-Amino-4H-chromenes are an important class of heterocyclic compounds having important biological activities. Many of the methods reported for the synthesis of these compounds are associated with the use of hazardous organic solvents, long reaction time, use of toxic amine-based catalysts, and lack of general applicability. Thus, the development of an inexpensive, mild, general, environmentally and commer Read More

In this work, two new prolinamides with isosteviol skeleton were synthesized and used as chiral catalysts for the asymmetric aldol reaction. Solvent effects, catalyst loading, substrate scope and the influence of water on the reaction were investigated. With only 5 mol % loading, the synthesized catalysts showed excellent activity (up to 98% yield) and good stereoselectivity (up to 87:13 dr, 90% ee) for the direct aldol reaction of c Read More

Background: Dibenzo-oxazepine and Benzothiazole derivatives are used as antipsychotics, anticancer, antibacterial and anti-inflammatory agents. Methods: Arylidene derivatives of 1,2,3,4-Tetrahydro-Dibenzo[b,f][1,4]Oxazepine and 2-[2-Chloro- Cyclohex-1-enyl]- Benzothiazoles were synthesized by reacting benzylidene derivative of chloroaldehyde with 2-aminophenol and 2-aminothiophenol respectively. Benzylidene Read More

Background: Brain cancer (neuroblastoma) and liver cancer (hepatocellular carcinoma) are common cancer types among others worldwide which do not have a radical treatment and cure. Objective: In the current study, five novel pyridazinone derivates bearing benzelhydrazone moiety at second position were synthesized and evaluated for their cytotoxic activity against neuroblastoma and hepatocellular carcinoma (SHSY5 Read More