Direct Asymmetric Reductive Amination

有机合成与工艺文献分享 2024-12-22 10:17

文章摘要

本文介绍了一种由默克研究人员开发的钌催化不对称直接还原胺化方法，用于从未保护的β-酮酰胺制备β-氨基酰胺。该方法通过酸添加剂（特别是水杨酸）来提高反应的活性和对映选择性，最终实现了高产率（96%）和接近完美的对映选择性（99.5% ee）。研究表明，过量的水杨酸铵不仅有助于平衡向产物方向移动，还能抑制二聚体的形成，从而提高产物的产率和选择性。该方法具有广泛的底物适用性，并已成功用于生产西格列汀，产率高达91%，具有前所未有的不对称诱导水平。

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