titoli, abstracts, parole chiave >>>
Synthesis of amides from aldehydes and amines via C-H bond activation and discovery and development of novel and selective carbonic anhydrase inhibitors

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.

[img]
Preview
Full text disponibile come PDF Richiede visualizzatore di PDF come GSview, Xpdf o Adobe Acrobat Reader
4Mb

Abstract

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.

Item Type:Doctoral Thesis
ID Code:10540
Contributors:Sechi, Mario and De Luca, Lidia Vera Giovanna
Publisher:Università degli studi di Sassari
Uncontrolled Keywords:Amides, CH activation, carbonic anhydrase inhibitors, benzoxaborole
Subjects:Area 03 - Scienze chimiche > CHIM/06 Chimica organica
Area 03 - Scienze chimiche > CHIM/08 Chimica farmaceutica
Divisions:001 Università di Sassari > 01-a Nuovi Dipartimenti dal 2012 > Chimica e Farmacia
Cicli, scuole e corsi:Ciclo 27 > Scienze e Tecnologie chimiche > Scienze chimiche
Deposited On:18 Mar 2015 13:13

I documenti depositati in UnissResearch sono protetti dalle leggi che regolano il diritto d'autore

Repository Staff Only: item control page