Here, we report a novel, efficient ruthenium-catalyzed direct asymmetric reductive amination of an α-alkoxy ketone, a structural motif for which it is more challenging to implement such a transformation than 1,3-dicarbonyl compounds. The discovery of a novel ruthenium catalyst that was highly stable to air and moisture, as well as being readily prepared from commercially available reagents, enabled rapid access to a key synthetic chiral primary amine en route to TAK-915, an active pharmaceutical ingredient for a PDE2A inhibitor.

中文翻译：

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用于合成 PDE2A 抑制剂 TAK-915 的手性伯胺中间体的钌催化直接不对称还原胺化

在这里，我们报告了一种新型、高效的钌催化的 α-烷氧基酮的直接不对称还原胺化，这是一种结构基序，实现这种转化比 1,3-二羰基化合物更具挑战性。一种对空气和湿气高度稳定的新型钌催化剂的发现，以及易于从市售试剂中制备的新型钌催化剂的发现，使人们能够快速获得关键的合成手性伯胺，从而获得 TAK-915，TAK-915 是一种药物活性成分PDE2A抑制剂。