Synthesis and biological activity of aminoacetyl and aminoethyl derivatives of indolo [1,2-c]quinazoline

First Total Synthesis of Hinckdentine A

“…The framework of 1 consists of biologically important dihydrotryptamine and dihydropyrimidine units together with a cataleptically active indolo[1,2- c ]quinazoline core, although the biological activity of 1 has not yet appeared in the literature. Structural and biological interests have attracted several organic chemists to attempt the synthesis of 1 .…”

Copper-Catalyzed Sequential Ullmann N-Arylation and Aerobic Oxidative C–H Amination: A Convenient Route to Indolo[1,2-c]quinazoline Derivatives

“…It is the core skeleton of the marine alkaloid hinckdentine A (Figure ), and its derivatives have shown interesting biological and pharmacological activities. For example, certain derivatives of indolo[1,2- c ]quinazoline present cataleptogenic activity, and some show excellent antibacterial as well as antifungal properties that make them promising drug candidates for Ampicillin and Ketoconazole …”

12-Acylindolo[1,2-c]quinazolines by Palladium-Catalyzed Cyclocarbonylation of o-Alkynyltrifluoroacetanilides

“…The presence of the indolo[1,2- c ]quinazoline skeleton in natural substances such as Hinckdentine A, an unusual marine alkaloid that has been isolated from the bryozoan Hincksinoflustra denticulata , as well as the biological activity exhibited by certain derivatives of indolo[1,2- c ]quinazoline, , prompted us to investigate further the cyclization of 1 to indolo[1,2- c ]quinazoline products and, possibly, the synthetic scope of the reaction.…”