This review summarizes the recent advances in the synthesis and biological activities investigations of quinazoline derivatives.
Other forms of this drug- Itraconazole and Fluconazole- have been produced to improve upon the number of side effects and effectiveness for certain types of infections.
Some fungi have shown resistance to Ketoconazole, such as Candida albicans.
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 .
Ketoconazole is an antifungal drug effective against fungus of the lymph nodes, skin, nails, respiratory system, bone, and other parts of your pet’s body.
A shampoo that mixes Ketoconazole with Chlorhexidine is used to treat fungal and bacterial skin infections.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.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.In addition, the bioactivity researches of quinazoline derivatives were also discussed in order to provide valuable reference for the future synthesis and biological investigation of these compounds.Imino-Diels-Alder reaction  containing the coupling of imine and electron-rich alkene gradually became a powerful tool for the synthesis of quinazoline derivatives .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 Povarov imino-Diels-Alder reaction, aniline and ethyl glyoxalate were chosen as substrates.And two molecules of  was extended from the Povarov Imino-Diels-Alder reaction.