Synthesis of α,α-Disubstituted Benzocyclobutane Amino Acids through [2+2] Annulation of Benzyne with Dehydroalanine

被引：6

作者：

Picard, Audrey ^{[1
]}

Ciblat, Stephane ^{[1
]}

Ramtohul, Yeeman K. ^{[1
]}

机构：

[1] Paraza Pharma Inc, 2525 Ave Marie Curie, St Laurent, PQ H4S 2E1, Canada

来源：

SYNLETT | 2020年 / 31卷 / 05期

关键词：

benzyne; aryne; dehydroalanine; alpha; alpha-disubstituted benzocyclobutane amino acids; peptidomimetic; ANALOGS;

D O I：

10.1055/s-0039-1691572

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A mild and general method for the synthesis of alpha,alpha-disubstituted benzocyclobutane amino acids through a [2+2] annulation of benzyne with dehydroalanine is described. Yields up to 88% of the constrained quaternary amino acids can be obtained and its application in peptidomimetic synthesis is demonstrated.

引用

页码：507 / 511

页数：5

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