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A novel base-mediated intramolecular hydroamination to build fused heteroaryl pyrazinones |
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| Authors: | Laura Llauger Costanza Bergami Olaf D Kinzel Samuele Lillini Giovanna Pescatore Caterina Torrisi Philip Jones |
| Institution: | Department of Medicinal Chemistry, IRBM-MRL Rome, Via Pontina Km 30,600, Rome 00040, Italy |
| Abstract: | Functionalized fused heteroaryl pyrazinones were built up through a novel DBU-catalyzed intramolecular hydroamination reaction of aryl(prop-2-yn-1-yl)-1H-heteroaryl-2-carboxamides. The nucleophilic addition afforded three isomers; two with an exo-cyclic double bond cis (Z), trans (E)], and a third one with an endo-cyclic double bond. After the carboxamide deprotection, isomerization of the mixture under acidic conditions resulted in a unique isomer. |
| Keywords: | Intramolecular hydroamination Pyrrolopyrazinones Fused-heteroaryl pyrazinones DBU-mediated cyclisation Isomerisation |
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