Synthesis of (Carbo)nucleoside Analogues by [3+2] Annulation of Aminocyclopropanes

With more than 45 FDA approved drugs, nucleoside analogues constitute one of the most important classes of bioactive compounds. Nevertheless, most synthetic methods are based on linear multi-step sequences, making the synthesis of structurally diverse libraries of nucleoside analogues difficult. The group of Professor Jérôme Waser from the Ecole Polytechnique Fédérale de Lausanne (Switzerland) reported a new method for synthesizing nucleoside analogues via a [3+2]-annulation reaction, using donor–acceptor cyclopropanes for the first time.

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