A mild and general method for the synthesis of α,α-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.

中文翻译：

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苯与脱氢丙氨酸的[2+2]环化合成α,α-二取代苯并环丁烷氨基酸

描述了一种通过苄与脱氢丙氨酸的 [2+2] 环化合成 α,α-二取代苯并环丁烷氨基酸的温和通用方法。可以获得高达 88% 的受限季氨基酸，并证明了其在拟肽合成中的应用。