Open Access Library Journal How to cite this paper: Hussein, A.H.M., Abu-Shanab, F.A. and Mousa, S.A.H.S. (2015) Benzoylacetone as a Building Block in Heterocyclic Synthesis: Synthesis of Polyfunctionally Substituted Pyridinethione and Its Derivatives. Open Access Library Journal, 2: e1274. http://dx.doi.org/10.4236/oalib.1101274 Benzoylacetone as a Building Block in Heterocyclic Synthesis: Synthesis of Polyfunctionally Substituted Pyridinethione and Its Derivatives Abdel Haleem Mostafa Hussein * , Fathi Ali Abu-Shanab, Sayed Abdel Hamed Sayed Mousa Department of Chemistry, Faculty of Science, Al Azhar University, Assiut, Egypt Email: * abdelhaleemmh@yahoo.com Received 5 January 2015; accepted 22 January 2015; published 26 January 2015 Copyright © 2015 by authors and OALib. This work is licensed under the Creative Commons Attribution International License (CC BY). http://creativecommons.org/licenses/by/4.0/ Abstract The Hantzsch amide derivatives 1 are prepared by reaction of a mixture of two moles of benzoy- lacetone, aqueous ammonia and aromatic aldehydes. Also, the reaction of benzoylacetone with a mixture of urea or thiourea and aromatic aldehydes afforded pyrimidine derivatives 2a-h. Pyridi- nethione derivative 3 was reacted with α–haloketones and α–halonitriles 4a-e to afford the S-alky- lated derivatives 5a-e which cyclized into 6b-e and 7. Reactions of compound 7 with glacial acetic acid/acetic anhydride gave 8 which led to 9a and 9b on treatment with ammonium acetate/acetic acid and aniline. Also, treatment of 7 with formamide, hydrazine hydrate and benzoyl isothiocya- nate afforded 10, 11 and 13. Reactions of 3 with arylidenemalononitrile 14 in ethanolic triethyla- mine yielded 1:1 addact 17a-c. Keywords Pyridines, Pyrimidines, Pyridinthione, Pyridothienopyrimidine and Isoquinolines Subject Areas: Analytical Chemistry, Organic Chemistry 1. Introduction Polyfunctionally substituted 1,4-dihydropyridines have been widely explored as cardiovascular agents. Nifedi- pine has been approved for clinical use as an antianginal agent and represents the prototype 1,4-dihydropyridine (DHP) structure found useful in both antianginal and antihypertensive therapy [1]. Also, the pyridinethione rings * Corresponding author.