Abstract

AbstractDynamic kinetic resolution is one of the most synthetically useful phenomena for asymmetric synthesis. Dynamic kinetic resolution for the catalytic asymmetric synthesis of a spiro[imidazo[1,2‐a]pyrazine‐2(3H),4′‐piperidin]‐5(1 H)‐one scaffold with a lanthanum‐linked BINOL complex is described. It is also clarified that starting materials, diamine 1 and keto ester 2, play important roles not only as substrates but also as additives to modify an active species of the lanthanum complex. The catalytic asymmetric total syntheses of our antithrombotic agents M58163 and M58169 have thus been achieved via dynamic kinetic resolution.

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