Multi-component synthesis of dihydropyrimidines by iodine catalyst at ambient temperature and in-vitro antimycobacterial activity.
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.
Zalavadiya
Paresh
P
Chemical Research Laboratory, Department of Chemistry, Saurashtra University, Rajkot Gujarat, India.
Tala
Satish
S
Akbari
Jignesh
J
Joshi
Hitendra
H
D000995:Antitubercular Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D002384:Catalysis; D004353:Drug Evaluation, Preclinical; D066298:In Vitro Techniques; D007455:Iodine / Q000737:chemistry*; D015394:Molecular Structure; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D011743:Pyrimidines / Q000138:chemical synthesis*; D013329:Structure-Activity Relationship; D013696:Temperature
D000995:Antitubercular Agents; D011743:Pyrimidines; D007455:Iodine