Tuesday, June 24, 2008 - 3:50 PM
New York (Capital Hilton)
41

A Clean, Benign and Aqua Mediated Synthesis of Pharamacologically Active Spiro Heterocycles

Subhash C. Jain, Siva Panda, Pankaj Khanna, and Sunita Bhagat. University of Delhi, Delhi, India

The Chemistry of spiro heterocycles has been of considerable interest due to their pharmacodyanamic nature and therapeutic importance. In continuation to our interest in the development of new bioactive heterocylces, we have recently found a clean, facile, ecofriendly and an economic route for the synthesis of some novel spiro heterocycles, viz. spiro[indol-pyrazolinyl-thiazolidines], spiro[indol-indozolyl-thiazolidines] and spiro[indol-benzooxazines] each containing different biodynamic moieties. These spiro heterocylces have been prepared via hitherto unknown Schiff's bases, which in turn were obtained by the reaction of indol-2,3-diones with various aromatic and heterocyclic amines, under aqueous conditions, in 90-98% yield. Further, a series of various biologically active symmetrical and unsymmetrical bis spiro indolyl compounds, containing alkyl and piperazinyl linkers, have also been synthesized using above developed methodology.

Some of these novel spiro heterocylces possessed anti-inflammatory, fungistatic, bacteriostatic and anti-convulsaint activities, therefore all the above synthetic compounds have been screened for a broad spectrum of biological activities, in order to discover new pharmacophores for the future. Detailed synthetic methodology as well as the bio-activity data will presented and discussed at the Conference.