Core Scaffold-Inspired Stereoselective Synthesis of Spiropyrazolones via an Organocatalytic Michael/Cyclization Sequence

[摘要]：Herein, the organocatalytic asymmetric Michael/cyclization sequence of alpha-isothiocyanato imides and esters with a variety of unsaturated pyrazolones is presented, in general, affording functionalized spiropyrazolones containing three contiguous stereogenic centers in high levels of diastereo- and enantioselectivity (up to 20:1 dr and 99% ee). Moreover, the current protocol provides a highly efficient and convenient strategy that allows rapid enantioselective construction of diversely spiropyrazolone skeletons with high optical purity.

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