Abstract
Abstract A concise total synthesis of CDK 4/6 inhibitor abemaciclib is described. The synthesis uses a Suzuki coupling, followed by a Hartwig–Buchwald amination to join three of the four subunits. The final step is a reductive amination utilizing Leuckart–Wallach conditions. Key to the Leuckart–Wallach reaction was the addition of trimethyl orthoformate to remove water formed during the reaction, allowing the reaction to go to completion.
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