A rapid one-pot solvent-free procedure has been developed for the synthesis of fluorinated 2,3-disubstituted quinazolin-4(3H)-ones by neat three-component cyclocondensation of anthranilic acid, phenyl acetyl chloride and substituted anilines under microwave irradiation. The experimental methodology and microwave conditions described here are well established, allowing significant rate enhancement and good yields compared to conventional reaction conditions. The reaction is generalized for o-, m-and p-substituted anilines with electron-donating and -withdrawing groups to give quinazolin-4(3H)-ones. Synthesized compounds have been screened for their anti-fungal activity. #
A simple and fast three-component diastereoselective synthesis of biologically important spiro scaffold 4 was carried out in reasonable purity starting from readily available 1H-indole-2,3-dione 1, ethyl cyanoacetate 2 and 4-hydroxycoumarin 3 under microwave in high yield (88%-92%) and short time.
Industries are constantly in search of efficient and green chemistry protocols for the synthesis of pyrimido [2,1-b]benzothiazoles. One-pot reaction of 2-aminobenzothiazole, active methylene derivatives, and carbonyl compounds expeditiously annulate a pyrimidine ring on the benzothiazole nucleus to yield pyrimido [2,1-b]benzothiazole under microwaves or ultrasonic waves using water as energy transfer medium. The title compounds are easily accessible by various approaches; even waste-free procedures have been developed. The operational simplicity, environmentally friendly conditions, and high yield achieved in a very short reaction time are major benefits that meet the requirements of green production, including saving energy and high efficiency. The results are compared with conventional heating. Structural assignments are based on spectroscopic data.
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