Herein, nucleophilic substitution reaction of pyrimidine derivatives on piperazine in ciprofloxacin resulted in the formation of new pyrimidyl N-ciprofloxacines. These compounds were prepared at room temperature, at conventional heating and under microwave irradiation conditions. Results indicated microwave condition as a green approach in comparison with room temperature and at conventional heating condition leads to higher yields and very short reaction times. 1 H, 13 C-NMR, FT-IR, Mass spectroscopy and CHN analysis were used to characterize all the synthesized products. Meanwhile, the antibacterial activity of these new compounds against gram-positive and gram-negative bacteria was investigated and showed more activities for two new N-ciprofloxacin derivatives than ciprofloxacin.[a] Dr.
Benzimidazolium based on dicationic acidic ionic liquid (AIL)is designed, synthesized, and successfully used as a catalyst for the one-pot synthesis of α-aminophosphonates derivatives. The application of this acidic ionic liquid is studied in a new one-pot method for the synthesis of α-aminophosphonates derivatives under solvent-free conditions. The advantages of this method are the reusability of the catalyst, high conversion, short reaction time, and simple experimental procedure.
Solvent-free synthesis of 3-substituted indole derivatives by a one-pot three-component coupling reaction between aldehyde, N-alkyl aniline and indole by Fe(HSO 4 ) 3 catalyzed is described. The noticeable features of this protocol are the simplicity of the procedure, easy synthesized, recyclable and inexpensive catalyst, no organic solvent and high yields in relatively short reaction times.
Scheme 1 Catalytic synthesis of 3-aminoalkylated indolescreasing the amount of catalyst from 10 to 5 mol % lowered the substrate conversion rate (Entry 12).Surprisingly, omitting the solvent made the reaction faster and a much better yield of desired indolylmethane
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