[Polymorphism of 3,9-bis-(N,N-dimethylcarbamoyloxy)-5H-benzofuro[3,2- c]quinoline-6-one(KCA-098), a new...

Physicochemical properties of polymorphism of 3,9-bis-(N,N-dimethylcarbamoyloxy)-5H-benzofuro[3,2-c]quinol ine-6-one (KCA-098) have been investigated. The existence of four crystalline forms (designated as hydrate, I, II and III) was confirmed by X-ray powder diffraction, IR spectroscopy and thermal analysis (DSC and TG). The hydrate was found to be a monohydrate by elemental analysis and water content measurement. DSC measurement found that the hydrate was transformed fo form III at about 93 degrees C, and then to form II at about 152 degrees C, and finally to form I at about 260 degrees C. On the other hand, when suspended in water the forms I, II and III were transformed into hydrate. The transition rate from form III to hydrate was higher than those from form II to hydrate and from form I to hydrate. Form III as a metastable form showed higher solubility than any of form I, II and hydrate.