Clortalidona (CTD): polimorfismo, enantiomeria e substâncias relacionadas

Abstract

In this work will be presented the four polymorphs of the diuretic and antihypertensive drug Chlorthalidone, (RS)-2-Chloro-5-(1-hydroxy-3-oxo2,3-dihydro-1H-isoindol-1-yl)benzene-1-sulfonamide (CTD) , noting that all of them were elucidated by the Group of Crystallography of the UNIFAL-MG and polymorph recently elucidated , is a direct result of the conduct of this work of Science Master. There will be correlation structure/properties of solid state to explain the differences in results obtained by the characterization of polymorphs I and II of the CTD by infrared spectroscopy and thermal analysis based on the intrinsic structural features of both polymorphs, showing as the phenomenon of polymorphism can impact and affect the physicochemical properties of a drug. Two novel crystal structures of 4’-chloro-3’-sulfamoylbenzophenone carboxylic acid (CCA) will also be presented. This is a hydrolysis product of CTD and also a biologically active compound that can act as a diuretic. Furthermore, synthetic routes that resulted in the formation of CCA and two other CTD related substances will be presented, as well as a mechanistic study that allows predict and propose the synthesis of other related compounds.