CHAPTER III BIGINELLI REACTION INTRODUCTION Dihydropyrimidinones (DHPMs), commonly known as Biginelli compounds, have attained unprecedented attention due to its greater biological, pharmaceutical and therapeutic properties. In 1893, Pietro Biginelli reported the first synthesis of 3,4-dihydroprimidin-2(1H)ones (DHPM) by a very simple multi-component one-pot condensation reaction of an aromatic aldehyde, urea and ethyl acetoacetate in ethanolic solution1 (Scheme 1.1). This efficient approach to partly reduced pyrimidines, termed the Biginelli reaction or condensation, was largely ignored in the following years, and therefore, also the synthetic potential of these multi-functionalized dihydropyrimidines remained unexplored. In recent years, however, interest in these compounds has increased rapidly, and the scope of the original cyclocondensation reaction has been widely extended by variation of all three components. Scheme 1.1. Classical Biginelli …show more content…
As early as 1930 simple derivatives such as 33 were patented as agents for the protection of wool against moths.52 Later, interest focused on the antiviral activity of Biginelli compounds,53 eventually leading to the development of nitractin (34), which has excellent activity against the viruses of the trachoma group.14,54 The Biginelli compounds also exhibits modest antibacterial activity. 55 Dihydropyrimidinone 1 and some of its analogs were screened as antitumor agents and found to be active against Walker carcinosarcoma in rats and mice.55-57 Pyrimidine 5-carboxamides of type 35 are reported to possess anticarcinogenic58 activity. Antinflammatory,9,59 antioxidant,59b analgesic,9 and blood platelet aggregation inhibitory activity 8 was found in a number of derivatives. 1,4 Dihydropyrimidine 36 is useful as platelet- activating factor antagonist.60 Other Biginelli compounds were shown to inhibit the uptake of adenosine by thrombocytes.
Cadet Eric Wiggins Date: 18 September 2014 Course Name: Chem 100 Instructor: Captain Zuniga Section: M3A Identification of a Copper Mineral Intro Minerals are elements or compounds that are created in the Earth by geological processes. The method of isolating metals in a compound mineral is normally conducted through two processes.
This week we went to the Conodoguinet Creek. While we were at the creek we did many different things. One of the experiments we did was the Critter Count which was my favorite. Another experiment we did was the Eutrophication Tests. The last Experiment we did was the bobber test.
Testing phase finds differences in positive/negative documents by the centroid obtained in training phase by ranking each of them. The simple way to estimate similarity between documents and centroid by summing weights of patterns which are in the documents. VII. Experimental Results To determine accurate measures of similarity or difference between documents you depict results by graph pattern and table pattern. The experimental setup consists of relevant documents that you termed as positive and negative documents .i.e
Name: Avishak Deb Roy Partners: Leevell Penn, Varugh, Butler Bio 101 Lab Report #1 02.22.2018 Swimming speed of paramecium tetraurelia in different levels of treatment. Introduction Paramecia is a unicellular Protista which are naturally found in aquatic habitats. It is easily cultured in the laboratory. It is oblong shaped and covered with short hairy structure called cilia. Paramecia does not pose any health or ethical concerns and the population can be maintained if there is a food source such as Enterobacter (Biological Foundation 7).
The lab started off by measuring critical materials for the lab: the mass of an an empty 100 mL beaker, mass of beaker and copper chloride together(52.30 g), and the mass of three iron nails(2.73 g). The goal of this experiment is to determine the number of moles of copper and iron that would be produced in the reaction of iron and copper(II) chloride, the ratio of moles of iron to moles of copper, and the percent yield of copper produced. 2.00 grams of copper(II) chloride was added in the beaker to mix with 15 mL of distilled water. Then, three dry nails are placed in the copper(II) chloride solution for approximately 25 minutes. The three nails have to be scraped clean by sandpaper to make the surface of the nail shiny; if the nails are not clean, then some unknown substances might accidentally mix into the reaction and cause variations of the result.
Prove if the material in cup 6 is a metal, metalloid, or nonmetal, by using its appearance, color, state of matter, luster, conductivity, malleability, and how it reacts with HCL. Before beginning to test on the substance we observed its appearance, state of matter, luster, and color. The substance was very shiny, solid and hard, as well as silver. Then we put on safety goggles to start testing.
Genetic engineering is changing the DNA code to express different traits. A plasmid is a circular piece of DNA that contains important genetic information. Recombinant DNA is the product after inserting your desired genes. The genes we hoped to insert in the pGLO lab were the GFP gene and the ampicillin resistance gene. GFP was needed so that we would tell if the ampicillin resistance gene had been properly placed when the bacteria glowed under a UV light.
The question is, how does a physical or chemical change affect the mass of a substance within a closed system? To respond to this question, my group did a lab to determine whether or not the mass would change or not. Our lab was to have a plastic bag containing baking soda, then add a cup of vinegar and a block of clay to the mix. We made sure to weight every element separately and then add them up for our total mass of 31 grams before the reaction. During the reaction, as soon as the vinegar was poured in there was a gas produced, bubbles.
Abstract In this experiment, the reaction kinetics of the hydrolysis of t-butyl chloride, (CH3)3CCl, was studied. The experiment was to determine the rate constant of the reaction, as well as the effects of solvent composition on the rate of reaction. A 50/50 V/V isopropanol/water solvent mixture was prepared and 1cm3 of (CH3)3CCl was added. At specific instances, aliquots of the reaction mixture were withdrawn and quenched with acetone.
SO2 responsible for CA inhibitory action of the compound. If R = OH, hCA 2 inhibitory activity is reduced.
Reactivity of Metals in Single-Replacement Reactions A lab was conducted to test the reactivity of metals in single-replacement reactions. This lab was done to solve the problem of which metals will replace each other in single-replacement reactions. A single replacement reaction is a type of oxidation-reduction chemical reaction when an element or ion moves out of one compound and into another. It was presumed before the experiment that the location of the metal on the Activity Series chart would thus determine the reactivity of the metal.
Title: THE BALLOON INFLATION REACTION Introduction: Chemistry is one thing that makes us understand and gives us reasons of why certain reactions gives certain results. In this experiment we will be illustrating the reaction between baking powder and vinegar and see what happens to the balloon that is attached to it. Hypothetically the reaction of the vinegar and baking powder will produce carbon dioxide which will inflate the balloon. If the more vinegar may happen that when more vinegar is added to the baking powder it may produce more carbon dioxide thus the balloons diameter increases.
The Wittig reaction is valuable reaction. It has unique properties that allows for a carbon=carbon double bond to form from where a C=O double bond used to be located. Creating additional C=C double bonds is valuable due to its use in synthesis. The Wittig reaction will allow the synthesis of Stilbene (E and Z) from a Benzaldehyde (Ketcha, 141).
Docking studies In the present study, the binding mode for novel 4-aminoquinoline-pyrimidine based molecular hybrids in the active site of wild type PfDHFR-TS and quadruple mutant PfDHFR-TS (N51I, C59R, S108 N, I164L) protein structures was explored using molecular docking studies. For this purpose, the prepared 3D structures of the compounds were docked in the binding pocket of both the wild type PfDHFR-TS and quadruple mutant PfDHFR-TS (N51I, C59R, S108 N, I164L) structures. The active aminoquinoline-pyrimidine conjugates interacted with wild and mutant PfDHFR-TS forming H-bond and π-π interactions.
also co-administration with antacids like magnesium hydroxide and aluminium hydroxide had no effect on oral absorption.[6] plasma protein binding level is 31% and the volume of distribution approximates to the total body water content of 40–50 L. Plasma elimination half-life is 3.4–7.4 h. Linezolid is metabolized to two inactive metabolites, an aminoethoxyacetic acid (metabolite A) and a hydroxyethyl glycine (metabolite B). The clearance rate (+SD) is 80+29 mL/min and by non-renal (65%) and renal mechanisms. Renal tubular reabsorption may occur. Aproportion of the dose is excreted unchanged in the urine. extensive work on the pharmacokinetics of linezolid at different doses and in different groups of patients have been done.