A Noyori reduction of racemic 1-Boc-3-fluoropiperidin-4-one has been achieved under dynamic kinetic resolution conditions that results in a single cis enantiomer being obtained with both diastereo- and enantioselectivity > 90%. This medicinal chemistry building block can be generated on multi-gram scale using the developed conditions to a single enantiomer in a 60% yield after employing a crystallisation procedure.

中文翻译：

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努力通过动态动力学拆分将No3-ori还原为3-fluorpiperidin-4-one

在动态动力学拆分条件下已实现了外消旋的1-Boc-3-氟哌啶丁-4-酮的Noyori还原，可得到单一的顺式对映异构体，其非对映体和对映体选择性均> 90％。在采用结晶程序后，可以使用开发的条件以60％的收率以单克对映体的形式，以多克级的规模生成这种药物化学组成部分。