期刊
TETRAHEDRON LETTERS
卷 56, 期 7, 页码 949-951出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tetlet.2014.12.082
关键词
Abemaciclib; Leuckart-Wallach reaction; Reductive amination; Hartwig-Buchwald coupling; Suzuki coupling
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. (C) 2014 Elsevier Ltd. All rights reserved.
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