Letters in Organic Chemistry - Volume 13, Issue 4, 2016

Background: Several crysene derivatives have been prepared using different protocols; however some require special reagents and conditions. The aim of study involved the synthesis of two crysene derivative using androsterone and estrone as chemical tool. Methods: Crysene derivatives were prepared by a series of reactions that involve; 1) Synthesis of two isoquinolinone derivatives by reaction of androsterone or estrone with Read More

Background: A series of novel 2-methoxy-N-phenyl-6-(5-phenyl-1,3,4-oxadiazol-2- yl)pyridin-3-amine (6a-i) have been synthesized from bromo methoxy picolinicacid as starting material. Finally, oxadiazole was coupled with various anilines using buchwald coupling reactions to give the target compounds. The newly synthesized compounds were evaluated for their efficacy as antimicrobial agents against various Gram-positive Read More

An environmentally benign protocol for the synthesis of some new 3, 4-dihydropyrimidin- 2-(1H)-ones and thiones promoted by p-Toulene Sulfonic Acid (PTSA) efficiently catalyzes the three component condensation reaction of formylchromone, substituted acetophenones and urea/thiourea under microwave irradiation (MWI). Compared to the classical Biginelli reaction conditions, this new methodology consistently has the ad Read More

Background: Thiazoles and their derivatives are attracting continuing interest over the years because of their varied biological activities. Thiazole and in particular the 2-amino thiazole moiety has been incorporated into a wide variety of therapeutically interesting candidates including antibacterial, anti-HIV, hypertension, anti-inflamenmatory, anti-viral and anticancer agents. Methods: Several methods for the synthesis Read More

Background: Structural distortions due to hyperconjugation in organic molecules, like norbornenes, are well captured through X-ray crystallographic data, but are sometimes difficult to visualize especially for those applying chemical knowledge and are not chemists. Methods: Crystal structure from the Cambridge database were downloaded and converted to .stI format. The structures were then printed at the desired scale usin Read More

Background: Marrubium vulgare is used in traditional medicine in some countries such as Jordan in the treatment of diabetes and wounds. The plant is reported to possess vasorelaxant, antihypertensive, analgesic, anti-inflammatory and antioxidant properties. Earlier phytochemical investigations of M. vulgare led to the characterization of the diterpene marrubiin (2) which is the major constituent of the plant [8], and Read More

Background: Cancer is a major health problem worldwide, the relative mortality rate caused by cancer is still very high in developed countries. Although the remarkable success has been achieved: more than 15 small molecule anticancer agents have been approved by the U.S. Food and Drug Administration (FDA) in clinics and dozens are currently in clinical trials, cancer chemotherapy is still highly inadequate, and it is ess Read More

Background: Benzodiazaphosphorines have many biological activities such as fungicidal and antitumor. In this work we are interested to synthesize them in order to test their activities in future work. The probable mechanism of obtained benzodiazaphosphorines is discussed. Methods: The obtained benzodiazaphosphorines were characterized using FT-IR, NMR 1H and 13C spectroscopy and elemental analysis. Results: A seri Read More

Background: With growing interest in developing environmentally friendly reactions and atom-economic processes in recent years, the utilization of water as a solvent has attracted a great deal of attention. This is not only for its low-cost, safe and environmentally benign nature, but also the unique properties of water in promoting reactions. Moreover, it may afford new access to the compounds that required harsh reaction c Read More

Background: Traditional Chinese medicines have attracted increasing interest as potential sources of novel drugs with a wide range of biological and pharmacological activities. The leaves of Antidesma acidum Retz. were used in traditional medicine for treatment of stomachache of children, digestion related issues and diabetes. Moreover, phytochemical investigations of this plant confirmed the presence of alkaloids, triterpe Read More

Backgroung: A new bile acids conjugates have been obtained from 3α-bromoacetoxy derivatives of lithocholic, deoxycholic and cholic acids with salicylic, acetylsalicylic or nicotinic acids. These new conjugates were confirmed by spectroscopic (1H-, 13C NMR, FT-IR) analysis, mass spectrometry (ESI-MS) and semiempirical methods (PM5) as well as in silico (PASS) studies. Methods: This work reports an original synth Read More

Background: Pyrazole is a simple aromatic ring an organic compound of the heterocyclic series that characterized five-membered ring structure which comprises located adjacent two nitrogen atoms and three carbon atoms. In recent years interest in the pyrazole chemistry excessively has increased due to many a wide range of properties. Because they have a wide range of specific properties such as biological activities, p Read More

Background: The indole ring system and 4H-Pyran derivatives are significant components in many drugs and pharmaceutical agents and spirooxindole containing both indole and pyran rings have been shown to possess a wide biological and pharmaceutical properties. Methods: We synthesized new derivatives of spirooxindole by a three-component reaction of isatin derivatives, malononitrile (or ethyl cyanoacetate) a Read More