Multi-Component Synthesis of Dihydropyrimidines by Iodine Catalyst at Ambient Temperature and in-vitro Anti mycobacterial Activity

作者：Zalavadiya Paresh; Tala Satish; Akbari Jignesh; Joshi Hitendra^*

来源：Archiv der Pharmazie, 2009, 342(8): 469-475.

DOI：10.1002/ardp.200800224

• Ambient temperature
• Antimycobacterial activity
• Molecular iodine
• 1-Substituted DHPMs
• Three-component domino synthesis

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.

• 出版日期2009-8