Vaccine Systhesis

Vaccine Systhesis-43
Store in a tightly sealed container at room temperature and protected from heat or light. If it is almost time for the next dose, skip the missed dose, and continue with the regular schedule. Ketoconazole may result in these side effects: Ketoconazole also blocks the systhesis of cortisone in the adrenal gland, which in some cases may be a harmful side effect, but when used correctly, it’s an effective treatment against Cushing’s syndrome.Owing to the significant biological activities, quinazoline derivatives have drawn more and more attention in the synthesis and bioactivities research.In Povarov imino-Diels-Alder reaction, aniline and ethyl glyoxalate were chosen as substrates.

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In this way, it was made possible for simple segregation of quinazolin-4-ones even with unquantitative cyclization reaction.

Compared to traditional heating methods, microwave heating could expand reaction range as well as shorten the reaction time from a few days or hours to a few minutes.

Quinazoline derivatives, which belong to the N-containing heterocyclic compounds, have caused universal concerns due to their widely and distinct biopharmaceutical activities.

Researchers have already determined many therapeutic activities of quinazoline derivatives, including anti-cancer [1-4], anti-inflammation [5,6], anti-bacterial [7-10], analgesia [5,9], anti-virus [11], anti-cytotoxin [12], anti-spasm [9,13], anti-tuberculosis [14], anti-oxidation [15], anti-malarial [16], anti-hypertension [17], anti-obesity [18], anti-psychotic [19], anti-diabetes [20], etc.

This review summarizes the recent advances in the synthesis and biological activities investigations of quinazoline derivatives.

According to the main method the authors adopted in their research design, those synthetic methods were divided into five main classifications, including Aza-reaction, Microwave-assisted reaction, Metal-mediated reaction, Ultrasound-promoted reaction and Phase-transfer catalysis reaction.The reactions were preceded in toluene as solvent and trifluorotoluene as co-solvent (Scheme ).After the reaction, desired products 15 were separated through solid-extraction on fluorous reversed-phase silica gel, for that the unreacted iminophosphoranes 13 and phosphane oxide 14 would leave the perfluoro tag on silica gel, thus make the products be washed off effectively.Thus, when applied in fields of organic synthesis, pharmaceutical chemistry and high-throughput chemistry, microwave heating shows greater advantage than traditional heating methods [28-31]. In their method, N’-(substituted-2-cyanophenyl)-N, N-dimethyl-formamidine derivatives and dialkyl amino (phenyl) were adopted as the raw materials to react in 4:1 volume ratio of isopropanol to acetic acid solvent for 20 min under microwave irradiation (100°C, 100 psi), and obtained twenty-four quinazoline compounds 18, two of which had similar activity as commercial reagent Ningnanmycin (Scheme .reported a fast, one-pot, microwave-assisted synthesis of polysubstituent imidazo[1,2-a]quinoline, pyrimido[1,2-a]quinoline and quinolino[1,2-a]quinazoline derivatives [33].The biological activities of the synthesized quinazoline derivatives also are discussed.This is an Open Access article distributed under the terms of the Creative Commons Attribution License ( which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.In this research, researchers chosed the same substrates as in the Povarov Imino-Diels-Alder reaction, and adopted various kinds of Lewis acid as catalysts, then the reagents were refluxed in toluene for one day, and finally produced quinazoline derivatives 3.Cu Br reported a kind of tandem Staudinger–Aza-Wittig–Nucleophilic addition reaction to synthesize indolo[1,2-c]quinazolines recently [25].This review summarized the representative synthetic methods, either traditional or novel, and categorized them into five main classifications, including Aza-reaction, Microwave-assisted reaction, Metal-catalyzed reaction, Ultrasound-promoted reaction and Phase-transfer catalysis.Besides, three other kinds of reactions were also listed out, which were either designed as supplementary methods in most experiments or used as the main methods in some researches, including Oxidative cyclization, Reagent refluxing and One-pot synthesis.


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