Current Organic Synthesis - Volume 16, Issue 1, 2019

Background: A lot of advancement has been made in the area of β-lactams in recent times. Most of the research is targeted towards the synthesis of novel β-lactams, their functionalization and exploring their biological potential. The C-3 functionalization of β-lactams has continued to attract considerable interest of the scientific community due to their utility as versatile intermediates in organic synthesis and their therapeutic Read More

Background: Heterocyclic compounds containing nitrogen have been known to possess a very important role in the field of medicinal chemistry. Indole and its derivatives displayed a wide range of biological properties such as anti-inflammatory, analgesic, anti-microbial, anti-convulsant, antidepressant, anti-diabetic, antihelmintic and anti-allergic activities etc. The diverse biological activities exhibited by compounds contai Read More

Background: Pentaerythritol (2,2-bis (hydroxymethyl) propane-1,3-diol) as white crystalline odorless solid has been synthesized in 1891. Pentaerythritol is multifaceted species in many compounds, which are wildly utilized in medicine and industry. Also, multicomponent reactions (MCRs) play a crucial role in organic and medicinal chemistry. Hence, in these reactions, pentaerythritol is a versatile substrate for the s Read More

Background: Enamines and their variant enamides as powerful and versatile synthons have attracted great attention in synthetic chemistry. Enamides display unique stability and reduce enaminic reactivity in view of the electron-withdrawing effect of N-acyl group. A great deal of satisfactory achievements in the synthesis and application of enamides has been made in recent years. Especially, tertiary enamides wit Read More

Halolactones are used both in chemical synthesis as intermediates as well as in various industries. These compounds may be secondary metabolites of living organisms, although they are mainly obtained by chemical synthesis. The substrates for the synthesis of chloro-, bromo- and iodolactones are often unsaturated carboxylic acids, and sometimes they are unsaturated esters. The article presents a number of diffe Read More

Background: 3,4-dihydroisocoumarins are an important small group belonging to the class of naturally occurring lactones isolated from different bacterial strains, molds, lichens, and plants. The structures of these natural compounds show various types of substitution in their basic skeleton and this variability influences deeply their biological activities. These lactones are structural subunits of several natural products and ser Read More

Aim and Objective: Because of the low abundance of 3,4-unsubstituted coumarins in plants combined with the complex purification process required, synthetic routes towards 3,4-unsubstituted coumarins are especially valuable. In the present work, we explore the possibilities of a solvent-free Green Knoevenagel condensation on various 2-hydroxybenzaldehyde derivatives and malonic acid without the use of toxic Read More

Aim and Objective: A novel and convenient transformation for the synthesis of benzodiazepines has been developed via catalytic cyclization reaction using ionic liquid supported on mesoporous silica nanoparticles- imprinted iron metal (Fe-MCM-41-IL) as a recyclable catalyst under mild conditions. Materials and Methods: For preparation of Fe-MCM-41-IL, FeCl3·6H2O was added to a mixture of distilled water, CTAB and Na Read More

Aim and Objective: KIT-5 nanoporous silica was functionalized with sulfonic acid and SO3H group has been immobilized on nanoporous KIT-5 silica support via in situ method to produce novel nanocatalyst as “KIT-5-Pr-SO3H”. The catalyst was fully characterized by FT-IR, SEM, EDXs, TEM, BET and TGA techniques. The surface morphology images approved that the nanocatalyst particle sizes are around 7-15 nm. The prepared c Read More

Background: Quinolines represent an important class of bioactive molecules which are present in various synthetic drugs, biologically active natural compounds and pharmaceuticals. Quinolines find their potential applications in various chemical and biomedical fields. Thereby, the demand for more efficient and simple methodologies for the synthesis of quinolines is growing rapidly. Objective: The green one-pot Friedlander Synt Read More

Aim and Objective: Some ferrocenyl derivatives are active in vitro and in vivo against cancer. Generally, ferrocenyl derivatives for cancer research have three key components: a ferrocene moiety, a conjugated linker that lowers the oxidation potential and some derivative (peptide, nucleobase and others) that can interact with biomolecules. Since the pyrimidine fragment can easily pass through the membrane into the cells and Read More

Aim and Objective: It is known that the Lamotrigine drug has anti-inflammatory activity. So it was the goal to prepare similar compounds containing fluorine atoms (fluorine-substituted 3,5-diamino-6-aryl- 1,2,4-triazines) as Lamotrigine drug analogs to evaluate them as an anti-inflammatory. Materials and Methods: The novel fluorine substituted 3,5-diamino-6-aryl-1,2,4-triazines as new Lamotrigine analogs were prepared via Read More

Aim and Objective: The synthesis of bipyridines, especially 2, 2’-bipyridines, remains challenging because the catalytic cycle can be inhibited due to coordination of bipyridine to transition metal. Thus, the development of efficient methods for the synthesis of bipyridines is highly desirable. In the present work, we presented a promising approach for preparation of bipyridines via a Pd-catalyzed reductive homocoupling reaction wit Read More

Aim and Objective: The Biginelli reaction, first reported in 1893, is one great example of the important multicomponent reactions reported from 1893. Under the same conditions, the influence of the common catalysts on the yield of the Biginelli reaction was investigated. Materials and Method: To a round-bottom flask equipped with a spherical condenser were added 1,3- dicarbonyl compound (1.0 eq), urea (1.45 eq), ar Read More