3-cyanoacetylindole as a building block in the synthesis of nonfused and fused pyridine, pyrimidine, diazepine and pyranone derivatives

The reaction of 3-cyanoacctylindole I with trichloroacetonitrile afforded trichloroll1cthylpropen-1-one derivative 3 which upon the reaction with an excess of trichloroacetonitrilc yielded the ditrichlorome-thylpyrimidine derivative 5. It was converted to a variety of pyrazolo 7, dihydrazino 9. and isoxazolo pyrimidine II derivatives. The enaminonitrile 2 was used as a substrate to form the pyridine 13, 14, 16, diazepine 20 and pyranone 22 as well as 1, 2, 4-triazolo-25. 1, 2, 3, 4-tetrazolo-27, and benzimidazolo-pyrimidine 29 derivatives

Structural and specific solvent effects on the kinetics of Alkaline hydrolysis of methylacrylate and methylmethacrylate esters

The rates of alkaline hydrolysis of methyl prop-2-enoic acid [methylacrylate] 1 and methyl-2-methyl-prop-2-enoic acid [methylmethacrylate] 2 were studied at temperatures ranging from 10 to 35 degree in two series of dioxane-water and acetone-water mixtures containing 10 to 75 percent by volume of the organic component. The rate constants were found to be higher in acetone-water mixtures and decreased with increasing the dielectric constant of the medium. The kinetic studies and application of the differential method show that the rate follows a second order kinetic equation, first order with respect to both ester and hydroxide ion and the reaction proceeds by a B[Ac2] mechanism. The distance of closest approach of solvent molecules to the activated complex b and the distance of closest approach of solvent molecules to the transition state G were computed

Uses of 4-phenyl-3-thiosemicarbazide in heterocyclic synthesis: synthesis of pyrazole, pyrazolo [3.2-c] 1, 2, 4 triazole and pyrimidine derivatives

4-phenyl-3 thiosemicarbazide has been used in a new approach for the synthesis of heterocyclic and fused heterocyclic compounds which have many applications as anticancer, antimicrobial, antitubercular and antibacterial agents. In the present work, the reactivity of 4-phenyl-3-thiosemicarbazide towards diethylmalonate, malononitrile, urea and thiourea to afford pyrazole, triazole and pyrimidine derivatives was described. It is widely realized that certain fused heterocyclic compounds [1-4] posses diverse therapeutic potentialities; thus, they show antitumor, antimicrobial, antitubercular as well as antibacterial [5-8] activities. Prompted by these facts, the use of 4-phenyl-3-thiosemicarbazide for the preparation of new fused heterocycles belonging to pyrazoles, pyrazolo-triazoles and pyrimidines was suggested