The Synthesis of Diverse Annulated Pyridines with 6-Membered Functionalized Saturated Cycles for Medical Chemistry Research

Abstract

The article describes a set of pyridines annulated with functionalized 6-membered saturated rings, which are attractive
building blocks for the synthesis of diversified compound libraries in medical chemistry. A certain array of compounds includes pyridines with condensed cyclohexane, piperidine and tetrahydropyran cycles containing keto-, amino-, carboxylic
groups, as well as fluorinated fragments. The synthesis of the compounds using the procedure previously developed by us
via CuCl2-catalyzed condensation of propargylamine with ketones was performed. The limits of application of this reaction
were further expanded and determined in this work compared to our previous results. Condensed pyridines, which proved
problematic or impossible to obtain by this method, were synthesized using othersynthetic pathways. Thus, the study offers
a number of new building blocks for use in drug discovery.