New access to racemic β3-amino acids

  • Nejman M
  • Śliwińska A
  • Zwierzak A
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Abstract

A general simple procedure having the potential for large scale preparations of racemic β3-amino acids has been developed. The procedure involves base-catalyzed Michael-type addition of sodium diethyl malonate to N-Boc-α-amidoalkyl-p-tolyl sulfones in tetrahydrofuran. Hydrolysis of the adducts by refluxing with 6 M aqueous hydrochloric acid affords β3-amino acid hydrochlorides in high yield and excellent purity. © 2005 Elsevier Ltd. All rights reserved.

Author-supplied keywords

  • Diethyl malonate
  • Michael-type addition
  • N-Boc imines

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Authors

  • Michał Nejman

  • Anna Śliwińska

  • Andrzej Zwierzak

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