Thermal [2+2] Cycloaddition of CF(3)-Substituted Allenynes: Access to Novel Cyclobutene-Containing alpha-Amino Acids

[摘要]：An efficient approach for the preparation of novel CF(3)-substituted cyclic alpha-amino acid derivatives fused with cyclobutene ring has been developed. The method is based on intramolecular thermal [2+2] cycloaddition of amino acid containing allenynes with internal triple bond obtained by successive [2,3]-sigmatropic rearrangement of propargyl-containing nitrogen CF(3)-ylides and Sonogashira derivatization of the triple bond.

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