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

Heterocyclic communications

article

Oleksiy S. Artamonov¹  Taras Bulda¹  Tkhe Kyong Fam²  Evgeniy Y. Slobodyanyuk¹  Dmitry M. Volochnyuk¹  Oleksandr O. Grygorenko² 

[1] Institute of Organic Chemistry, National Academy of Sciences of Ukraine;National Taras Shevchenko University of Kyiv

关键词: amino acids;    conformational restriction;    lead-oriented synthesis;    oxazoles;    peptidomimetics;   

DOI  :  10.1515/hc-2015-0137

学科分类：内科医学

来源: De Gruyter

【 摘 要 】

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.

【 授权许可】

CC BY|CC BY-NC-ND