Asymmetric Total Synthesis of (S)-(+)-Cocaine and the First Synthesis of Cocaine C-1 Analogs from N-Sulfinyl beta-Amino Ester Ketals

[摘要]：Sulfinimine-derived alpha,beta-unsaturated pyrrolidine nitrones, on heating with Al(O-t-Bu)(3), undergo a highly stereoselective intramolecular [3 + 2] cycloaddition to give tricyclic isoxazolidines, which are transformed in three-steps to give C-1 substituted cocaine analogs.

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