An efficient and simple three-component domino synthesis of some new dihydropyrimidines (DHPMs) from aromatic aldehydes, 1,3-dicarbonyl compounds and N-(3-chloro-4-fluorophenyl)urea using molecular iodine as catalyst is described. The 1-substituted dihydropyrimidines were isolated in good to excellent yields (78-90%) within a short reaction time (4-6 h) at ambient temperature. The biological evaluation revealed that the newly synthesized compounds (4a-i and 5a-i) exhibited moderate antimycobacterial activity against Mycobacterium tuberculosis H(37) RV.

An improved method for the synthesis of some new dihydropyrimidines from aromatic aldehydes, 1,3‐dicarbonyl compounds, and thiourea with significant enhancement in reaction rates, short reaction time (4–6 h), good to excellent yields (70–93%), and ambient temperature using molecular iodine as catalyst is described. The biological evaluation revealed that the newly synthesized compounds 4a, 4b, 4c, 4d, 4e, 4f, 4g, 4h, 4i, 4j and 7a, 7b, 7c, 7d, 7e, 7f, 7g, 7h, 7i, 7j exhibited good antimicrobial activity and moderate antimycobacterial activity against Mycobacterium tuberculosis H37RV.

Activity. -A iodine-catalyzed Biginelli reaction is presented. All products are screened against Mycobacterium tuberculosis, but exhibit only weak activity compared to the standard drug rifampin. (IVa) is the most active derivative. -(ZALAVADIYA, P.; TALA, S.; AKBARI, J.; JOSHI*, H.; Arch. Pharm. (Weinheim, Ger.) 342 (2009) 8, 469-475; Dep. Chem., Saurashtra Univ., Rajkot 360 005, India; Eng.) -H. Haber 49-165

Activity. -The formation of dihydropyrimidines (IV) and (VII) from dicarbonyl compounds, aromatic aldehydes, and thiourea derivatives occurs with significant enhancement with regard to reaction rates, reaction time, and yield by using molecular iodine as the catalyst. Dihydropyrimidines (IV) and (VII) reveal good antimicrobial activity and moderate antimycobacterial activity against M. tuberculosis H 37 RV. -(ZALAVADIYA, P. D.; GHETIYA, R. M.; DODIYA, B. L.; VEKARIYA, P. B.; JOSHI*, H. S.; J. Heterocycl. Chem. 50 (2013) 4, 973-978, http://dx.