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
收藏
页码：507 / 511
页数：5
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