A versatile, facile and concise approach to access to highly substituted functionalized 2-(pyrrolidin-1-yl)thiazole ring system is accomplished. The efficient protocol proceeds by the reaction of corresponding racemic or enantiomerically enriched pyrrolidines and readily available benzoylisothiocyanate in acetonitrile followed by sequential reaction of readily available alpha-bromo ketones in acetone. The selectivity and good yield in the desired product is another important advantage of this reaction protocol. In a few cases, the resulting Nbenzoylthiourea intermediate cyclizes spontaneously before reacting with the benzophenone component. Finally, a wide study of the biological scope of this new bisheterocyclic molecules is reported.
Platinum complexes derived from two families of bidentate funcionalized aroylaminocarbo-N-thyoyl prolinates are prepared using mild conditions from prolinates, which are available via 1,3-dipolar cycloadditions. The resulting four coordinated neutral square-planar platinum(II) complexes are very stable and are fully characterized. Their structures are determined by spectroscopic and analytical methods and one of them by single crystal X-ray diffraction analysis. In this pattern, the platinum exhibits distorted square planar geometry, with cis-bond angles ranging from 89.42(2) and 94.37(6)° and trans-bond angles of 176.19(6) and 177.08(6)°, respectively. Anti(myco)bacterial and antifungal studies of all these new compounds are carried out under standardized protocols.
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