Synthesis, characterization and reactivity of cyclic and alicyclic sulfones.

PELÁEZ, W. J.

Teresina, Piauí

Simposio; Conferencista Invitado. II Encontro Estrategico de Ciencias Farmaceticas. II Seminario Ibero Americano de P y D de Medicamentos; 2015

Universidada Federal de Piauí - Facultad de Farmacia

Abstract. The synthesis of thio-ethers which can be oxidized to sulfones as provide to be a good methodology to obtain new heterocycles.1 In addition, these interesting compounds can be subjected to flash vacuum pyrolysis (FVP), microwave induced pyrolysis (MWIP) and conventional heating to carry out the extrusion of sulfur dioxide to generate intermediates that can be studied as new versatile building blocks.2 Between others, sulfonyl derivatives are structures with well-known biological activities.3 In particular, benzene-sulfonyl (BS) group is a substituent frequently present in biologically active molecules.3 Its presence leads to analogues with similar or better biological activities than their precursors.4 Recently, it was demonstrated that BS-tetrahydroquinolines possess anti-parasitic activity, while others have shown different behaviors as HIV-transcriptase inhibitors.4 On the other hand, the utilization of trifluoromethyl-sulfonyl (FMS) group as activator of pyridines to perform derivatizations is a well know methodology. Nevertheless, the elimination of this group with the objective to re-establish the aromatic system is not easy to carry out.5 As part of our ongoing project on thio-ethers, sulfoxides and sulfones as intermediates that allow us to obtain new bioactive heterocycles, our research has been focused on exploring the consequences of a sulfone-N and sulfone-C linkage on the stereoelectronic properties of some pyridines, quinolines and pirrolo-thiazoles.