A Simple, Efficient, and Highly Enantioselective Synthesis of MS-153 Employing a Chiral Silane Lewis Acid-Promoted Acylhydrazone-Enol Ether [3+2] Cycloaddition
作者： Kristy Tran , James L. Leighton
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摘要: Our previously reported chiral silane-promoted enol ether-acylhydrazone [3+2] cycloaddition reaction has been applied to a brief and efficient synthesis of the neuroprotective agent MS-153. Unsatisfactory variable levels efficiency enantioselectivity with requisite acetaldehyde-derived acylhydrazone occasioned modification silane Lewis acid, which led key step proceeding excellent (85 % yield) (≥98 % ee).
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