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

被引：2

作者：

Artamonov, Oleksiy S. ^{[2
]}

Bulda, Taras ^{[2
]}

Fam, Tkhe Kyong ^{[1
]}

Slobodyanyuk, Evgeniy Y. ^{[1
,2
]}

Volochnyuk, Dmitry M. ^{[2
]}

Grygorenko, Oleksandr O. ^{[1
]}

机构：

[1] Natl Taras Shevchenko Univ Kyiv, UA-01601 Kiev, Ukraine

[2] Natl Acad Sci Ukraine, Inst Organ Chem, UA-02660 Kiev, Ukraine

来源：

HETEROCYCLIC COMMUNICATIONS | 2015年 / 21卷 / 06期

关键词：

amino acids; conformational restriction; lead-oriented synthesis; oxazoles; peptidomimetics; NATURAL-PRODUCTS; DRUG DISCOVERY; ASYMMETRIC HYDROGENATION; RECEPTOR ANTAGONISTS; ORGANIC-SYNTHESIS; NICKEL CATALYSIS; EVOLVING ROLE; OXAZOLE; ESTERS; STEREOISOMERS;

D O I：

10.1515/hc-2015-0137

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

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.

引用

页码：391 / 395

页数：5

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