Der Pharma Chemica
Journal for Medicinal Chemistry, Pharmaceutical Chemistry and Computational Chemistry


Green synthesis of biginelli products of meldrum acid

Author(s): Vijay V. Dabholkar, Mustaqeem Mohammed A., Navnath B. Shinde, Omprakash G. Yadav

A simple and efficient method has been devised for the synthesis of 3,3-dimethyl-7H,8H,10H-8,10-diaza-2,4-dioxa- 5,9-dioxo-7-(substituted) phenylbicyclo [4.4.0] dec-1(6)-ene (5) and 3,3-dimethyl-7H,8H,10H-8,10-diaza-2,4-dioxa- 5-oxo-9-thioxo-7-(substituted) phenylbicyclo [4.4.0] dec-1(6)-ene (6), by a one-pot three component cyclocondensation reaction of 1,3 dicarbonyl compound (Meldrum), aromatic aldehyde, and urea/thiourea using catalytic amount of fresh lemon juice in refluxing ethanol. Representative samples were screened for their antimicrobial activities against gram-negative bacteria and gram-positive bacteria using disc diffusion method. The structures of the products were confirmed by IR, 1H, 13C NMR and elemental analysis.

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