Abstract
AbstractIn this report, two distinctive intramolecular cyclizations of o‐propargyloxy diketopiperazines (achieved from a one‐pot Ugi post‐transformation) is achieved via a copper(I)‐catalyzed intramolecular reaction of azomethine ylide and alkyne moiety. The presence of internal alkyne in the starting materials directed the reaction towards through [3+2]‐cycloaddition, while terminal alkyne led to a spirocyclization reaction between azomethine ylide and terminal unsaturated C−C bond. This method offering an opportunity for the synthesis of challenging Diazabicyclics and Spiro‐Diketopiperazinochromanes in high yields with exclusive diastereoselectivity.magnified image
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