A stereolibrary of conformationally restricted amino acids based on pyrrolidinyl/piperidinyloxazole motifs

作者：Artamonov Oleksiy S; Bulda Taras; Fam Tkhe Kyong; Slobodyanyuk Evgeniy Y; Volochnyuk Dmitry M; Grygorenko Oleksandr O^*

来源：Heterocyclic Communications, 2015, 21(6): 391-395.

DOI：10.1515/hc-2015-0137

• amino acids
• conformational restriction
• lead-oriented synthesis
• oxazoles
• peptidomimetics

A stereolibrary of conformationally restricted oxazole-containing amino acids, namely all isomers of 5-pyrrolydinyl- and 5-piperidinyloxazole-4-carboxylic acids, were designed and synthesized in three steps by the reaction of the corresponding N-Boc-protected amino acids and ethyl isocyanoacetate. These natural products-inspired amino acids are valuable building blocks for the synthesis of peptidomimetics and potential lead compounds for drug discovery.

• 出版日期2015-12