Abstract:A new spirocyclic amino acid for drug discovery, a surrogate for l‐proline/pipecolic acids, is described. The synthesis of multifunctional spirocycles starts from the commonly available cyclic carboxylic acids, for example, cyclobutane carboxylate, cyclopentane carboxylate, and l‐proline. The whole sequence includes only two chemical steps: synthesis of azetidinones and reduction into azetidines. The obtained spirocyclic amino acids were incorporated into a structure of the known anesthetic drug bupivacaine. T… Show more
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