Part –V: Utilities of Active Methylene Compounds and Heterocycles Bearing Active Methyl or having an Active Methine in the Formation of Nitrogenous Heterocycles Having oxygen or sulfur atom


  • Mohamed Abdel-Megid Chemistry Department, Faculty of Education, Ain-Shams Universit, Roxy,11711, Cairo, A.R. Egypt


Thiazepines, Oxazepines, Pyrans, Thiazines, Thiadiazoles, Oxadiazoles, Thiazoles, Isoxazles, Active methylene


Most of the common and novel synthesized active methylene compounds as well as heterocycles bearing active methyl or having methine site were used in the syntheses of wide variety of five-, six- and seven-membered azaheterocyclic systems having oxygen or sulfur atom in their structures in addition to some oxygenated heterocycles such as pyrans. Many synthetic approaches were used for the preparation of target heterocyclic systems such as cyclocondensation reactions, ring opening-ring closure, cycloaddition, acid-, base-catalyzed reaction, intermolecular cyclization and self-condensation as well as ring–chain tautomerism has been reviewed in this paper.


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Author Biography

Mohamed Abdel-Megid, Chemistry Department, Faculty of Education, Ain-Shams Universit, Roxy,11711, Cairo, A.R. Egypt

College of science and humanities at Hyrmmila, Shaqra University, KSA


Abass, M., Abdel‐Megid, M., & Hassan, M. (2007). Substituted Quinolinones, Part 12: Heterocyclization Reactions of 3‐(3‐Chromonyl)acryloylquinolinone with Some Bifunctional Nucleophiles. Synthetic Communications, 37(2), 329-352. doi: 10.1080/00397910601033930

Abdel-Megid, M. (1995). Synthesis of some new polynuclear heterocycles derived from ethyl α-[5-cyano 2-methyl-6-phenylpyrimidin-4-yl] cyanoacetate. Indian Journal of Heterocyclic Chemistry, 4, 269-272.

Abdel-Megid, M. (1997). ChemInform Abstract: Synthesis of Some Heterobicyclic Compounds Bearing 4-Anisyl-5-cyano-2- methyl-6-oxopyrimidin-1-yl Moiety. ChemInform, 28(35). doi: 10.1002/chin.199735039

Abdel-Megid, M. (2003). Reactivity of Functionally Substituted Azoles Towards Electrophiles. Novel Synthesis of Thienylazoles and Phenylazoles. Synthetic Communications, 33(1), 153-160. doi: 10.1081/scc-120015571

Abdel-Megid, M. (2006). A versatile molecule for the synthesis of some new polynuclear bioactive heterocyclic systems. International Journal of Chemistry, 16(3), 149-157.

Abdel-Megid, M. (2007). A New Route for the Synthesis of Substituted Pyridazines. Synthetic Communications, 37(18), 3211-3218. doi: 10.1080/00397910701547847

Abdel-Megid, M., Abass, M., & Hassan, M. (2007). Substituted quinolinones. Part 13 a convenient route to heterocyclization reactions with 3-substituted 4-hydroxyquinolin-2(1H)-one. Journal of Heterocyclic Chemistry, 44(2), 315-322. doi: 10.1002/jhet.5570440206

Abdel-Megid, M., Abdel-Rahman, T. M., & Ali, U. F. (1998). Synthesis of some aminopyrimido[4,5-d]pyrimidinethiones and related compounds with their effect of cellobiase activity. Mansoura Science Bulletin (A, Chemistry), 25(2), 17-35.

Abdel-Megid, M., Awas, M. A. A., Seada, M. H., Elmhdy, K. M., & Elsayed, M. M. (2010). Synthesis and Mollucicidal Activity of Some New Bicyclic and Polycyclic Pyrimidine Derivatives.

Abdel-Megid, M., Elkazak, A. M., Seada, M., & Farouk, O. (2010). Heterocyclization Reactions of 2-Arylideneamino-4,5-Diphenylfuran-3-Carbonitriles. Journal of Applied Sciences Research, 6(12), 2133-2138.

Abdel-Megid, M., Elnagdi, M. H., & Negm, A. M. (2002). Studies with 1-functionally substituted alkyl azoles: Novel synthesis of functionally substituted azolylbenzimidazoles and functionally substituted azolyl-1,2,4-triazoles. Journal of Heterocyclic Chemistry, 39(1), 105-108. doi: 10.1002/jhet.5570390115

Abdel-Megid, M., Gabr, Y., Awas, M. A. A., & Abdel-Fatah, N. M. (2009). Synthesis of some new hetarylpyranopyridazines, cinnolines, and hetarylpyridazine derivatives. Chemistry of Heterocyclic Compounds, 45(11), 1354-1364. doi: 10.1007/s10593-010-0433-1

Abdel-Megid, M., & Ismail, M. M. (2002). Synthesis of bioactive aza-heterocyclic systems derived from novel biheterocyclic enone. International Journal of Chemistry, 12(40), 287-296.

Abdel-Megid, M. H., Awas, M. A. A., Seada, M. H., El-Mahdy, K. M., & Elsayed, M. M. (2009). A Convenient Synthesis of Some New Bioactive Diheterocylic Thioether and Thiazolopyrimidine Derivatives. Acta Chem. Solv., 56, 852-859.

Brimble, M. A., Gibson, J. S., & Sperry, J. (2008). 7.08 - Pyrans and their Benzo Derivatives: Synthesis. In A. R. Katritzky, C. A. Ramsden, E. F. V. Scriven & R. J. K. Taylor (Eds.), Comprehensive Heterocyclic Chemistry III (pp. 419-699). Oxford: Elsevier.

Crossley, J. A., & Browne, D. L. (2010). An Alkynyliodide Cycloaddition Strategy for the Construction of Iodoisoxazoles. The Journal of Organic Chemistry, 75(15), 5414-5416. doi: 10.1021/jo1011174

el-Feky, S. A., & Abd el-Samii, Z. K. (1995). Synthesis and antiinflammatory properties of some novel thiazolidinones and imidazolidinones derived from 4-(3-phenyl-4(3H)-quinazolinon-2-yl)-3-thiosemicarbazone. Die Pharmazie, 50(5), 341-343.

El-mahdy, K., El-Kazak, A., Abdel-Megid, M., Seada, M., & Farouk, O. (2009). Synthesis, Characterization and Biological Evaluation of some New Thieno[2,3-d]Pyrimidine Derivatives. JOURNAL OF ADVANCES IN CHEMISTRY, 5(1), 581-591. doi: 10.24297/jac.v5i1.937

Gabr, Y., Abdel-Megid, M., Awas, M. A., & Abdel-Fatah, N. M. (2010). Synthesis of Some New Pyridazinylspirohetarylindoles and Hetarylpyridazine Derivatives. Heterocycles, 81(2), 395 - 406. doi: 10.3987/COM-09-11845

Ibrahim, M. A., Abdel-Hamed, M. A.-M., & El-Gohary, N. M. (2011). A new approach for the synthesis of bioactive heteroaryl thiazolidine-2,4-diones. Journal of the Brazilian Chemical Society, 22, 1130-1139.

Ismail, M. M., Abdel-Megid, M., & Hassa, M. M. (2004). Some Reactions of 2- and 4-Substituted 8-Methylquinolin-2(1 )-ones and their Thio Analogue. Chemical Paper, 58(2), 117-125.

Joule, J. A., & Mills, K. (2013). Heterocyclic Chemistry (Fifth ed.): John Wiley & Sons.

Kaur Manjal, S., Kaur, R., Bhatia, R., Kumar, K., Singh, V., Shankar, R., . . . Rawal, R. K. (2017). Synthetic and medicinal perspective of thiazolidinones: A review. Bioorganic Chemistry, 75, 406-423. doi:

Kishor, R. (2017). Review on Synthetic Routes for Synthesis of Benzofuran-Based Compounds Kishor R More. Journal of Chemical and Pharmaceutical Research, 9(5), 210-220.

Lakhan, R., & Singh, R. L. (1991). Synthesis and evaluation of 2-imino-3-(4-arylthiazol-2-yl)-4-thiazolidinones and their 5-arylidene derivatives as potential fungicides. Journal of Agricultural and Food Chemistry, 39(3), 580-583. doi: 10.1021/jf00003a029

M. Abdel-Megid, & M.A.A. Awas. (2002). A FACILE SYNTHESIS OF P-BIS(4-THIAZOLIDINON-3-YL)PHENYLENES AND RELATED SYSTEMS AND RELATED SYSTEMS. Heterocyclic Communications, 8(2), 161. doi:

Muylaert, K., Jatczak, M., Mangelinckx, S., & Stevens, C. (2016). Synthesis of pyrido-annelated diazepines, oxazepines and thiazepines. Current Medicinal Chemistry, 23(42), 4784-4823.

Seada, M., Abdel-Megid, M., & El-Deen, I. M. (1993). Synthesis and biological activities of some new thiazolidinones. Indian Journal of Heterocyclic Chemistry, 3, 81-86.

Seada, M., Fawzy, M. M., Jahine, H., Abd El-Megid, M., & Saad, R. R. (1989). Synthesis and Biological Activities of Some New Pyridazine Derivatives. Journal of the Chinese Chemical Society, 36(3), 241-249. doi: 10.1002/jccs.198900036

Seada M., Abdel-Rahman M. R., & Abdel-Megid M. (1993). Synthesis of some more 1,3-disubstituted-2,3-dihydro-2-thioxo-4,6-(1H,5H) pyrimidinediones and related analoges. Indian Journal of Heterocyclic Chemistry 3, 9-14.

Weinreb, S. M., & Orr, R. K. (2008). 8.07 - 1,2-Thiazines and their Benzo Derivatives. In A. R. Katritzky, C. A. Ramsden, E. F. V. Scriven & R. J. K. Taylor (Eds.), Comprehensive Heterocyclic Chemistry III (pp. 513-566). Oxford: Elsevier.




How to Cite

Abdel-Megid, M. . (2020). Part –V: Utilities of Active Methylene Compounds and Heterocycles Bearing Active Methyl or having an Active Methine in the Formation of Nitrogenous Heterocycles Having oxygen or sulfur atom. To Chemistry Journal, 7, 74-95. Retrieved from



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