Cadoni, Roberta (2015) Synthesis of amides from aldehydes and amines via C-H bond activation and discovery and development of novel and selective carbonic anhydrase inhibitors. Doctoral Thesis.
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This doctoral dissertation consists of two chapters.
In the first chapter is described the methodology developed for the synthesis of amides from aldehydes and amines by activating the aldehyde C-H bond. The technique involves the formation of N-chloro amine in situ, without being isolated from the reaction mixture, to which is then added the aldehyde. The two reagents in the presence of TBHP and Cu(OAc)2, forming the new CN bond. The method allowed to synthesize amides variously substituted in good yields.
In the second chapter is detailed a project focused on the development of new original and selective carbonic anhydrases inhibitors. This chapter is divided into four topics which include a) the application of the click chemistry as a powerful synthetic approach for the generation of sulfonamide-based inhibitors; b) the synthesis of a set of derivatives belonging to a previously indentified hit compound bearing the trifluorodihydroxypropanone moiety, and the strategy adopted for its biological optimization; c) the design and development of novel pyrazole-carboxylic acids derived from a previously identified lead compound, as well as its pharmacobiological optimization; d) the synthesis of potential carbonic anhydrase inhibitors carrying a benzoxaborole scaffold.
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