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Efficient microwave-assisted synthesis of 4-amino-2-benzazepin-3-ones as conformationally restricted dipeptide mimetics
Authors:Beatrice Severino
Institution:Dipartimento di Chimica Farmaceutica e Tossicologica, Università di Napoli, Federico II, Via D. Montesano, 49, 80131 Napoli, Italy
Abstract:In this paper, we describe the synthesis of conformationally constrained dipeptide mimetic derivatives. Microwave flash heating was used in several synthetic steps providing the opportunity to perform the reactions in dramatically shortened time as well as to increase the obtained yields. The efficiency of the methodology makes it useful in order to prepare other dipeptides containing the 4-amino-tetrahydro-2-benzazepin-3-one motif.
Keywords:Peptide mimetic  Constrained amino acids  Microwave irradiation  Intramolecular  Friedel-Crafts cyclization
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