Možnosti syntézy 2-fenylbenzothiazolů s potenciálním využitím v terapii rakoviny a PET zobrazování

Frydrych, Jan

Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Chemistry and Drug Control Candidate: Jan Frydrych Supervisors: Assoc. Prof. RNDr. Veronika Opletalová, Ph.D. Dr. Andrew Westwell Ph.D. Title of diploma thesis: Synthetic routes to 2-phenylbenzothiazoles with potential application in cancer therapy and PET imaging There are three main tasks reported in this thesis. The first is the report of an improved procedure for synthesis of biologically relevant 2-phenylbenzothiazoles with various substituents on phenyl ring. Reported 2-phenylbenzothiazoles were synthesised by heating equimolar amounts of 2-aminothiophenol disulfides with appropriate benzaldehydes with p-toluenesulfonic acid in the presence of polymer-bound triphenylphosphine using mixture of toluene and DMF as a solvent. Main features of reported method include simple product isolation (removal polymer-bound by-product by filtration through Celite® layer), avoidance of column chromatography, rapid synthesis and good yields of correspondent benzothiazole. The second goal of this thesis is the solution phase synthesis of 2-phenylbenzothiazoles bearing different substituents on both the benzothiazole and phenyl ring. Attempts were made to synthesise different 2-phenylbenzothiazoles by heating...

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