critical and rate-limiting step in the development process and present great potential for new enabling technologies and innovations. In this regard, there have been exciting advancements in the medicinalchemistry optimization toolbox. For example
Authors:Klára Lövei, István Greiner, János Éles, Áron Szigetvári, Miklós Dékány, Sándor Lévai, Zoltán Novák and György István Túrós
In medicinal chemistry, the development of synthetic procedures for the access of new heterocyclic systems as potential scaffolds is elementary. Herein, we report our results on the formation of small drug-like heterocycles, utilizing flow chemistry. This approach enables the extension of the reaction parameter window, including high-pressure/high-temperature or hazardous chemistry. In our work, various novel condensed tricyclic benzothiazoles fused with furo- and thieno-rings were synthesized applying a multistep continuous-flow protocol. The process includes two ring closure steps and a nitro group reduction step. Batch and telescoped continuous-flow syntheses were also designed and performed.
Authors:L. Fuks, E. Gniazdowska, P. Kozminski and J. Mieczkowski
Technetium(I) tricarbonyl complexes may form with the pyridine aldehyde thiosemicarbazones (TSCs), in which chelating ligand
is bound tri- or bidentately. Intend of the presented work was to check, if labeling the N-heterocyclic TSCs with tricarbonyl [99mTc]-technetium(I) may lead to formation of the complexes suitable for the radiopharmaceutical purposes. Syntheses of the complexes
were provided in the conditions analogous to those performed in the nuclear medicine laboratories. Main physicochemical properties
of the complexes important in the medicinal chemistry were studied. Relevant results of the numerical calculations remain
in fair agreement with these properties.
Vic-dioxime ligandsand their metal complexes are used in analytical, bio, pigment and medicinal chemistry. Complexes of nickel(II),
copper(II), and cobalt(II) with benzylamino-p-chlorophenylglyoxime (BpCPG) are synthesised. Thermal behaviour of these complexes was studied in dynamic nitrogen atmosphere by DTA, DTG and TG techniques.
GC-MS combined system was used to identify the products during pyrolytic decomposition. The pyrolytic end products were identified
by X-ray powder diffraction. Thermoanalytical data of these complexes are presented in this communication. Interpretation
and mathematical analysis of these data and evaluation of order of reaction, the energy and entropy of activation based on
the integral method using the Coats-Redfern equation and the approximation method using the Horowitz-Metzger equation are
also given. The metal complexes undergo decomposition in three stages and metal oxides remained as end products of the complexes.