An alternative route toward enantiomerically highly enriched N-acyl amino nitriles based on the Cu(OAc)₂-catalyzed dehydration of aldoximes, which are readily available from N-acyl l- or d-α-amino aldehydes through condensation with hydroxylamine, has been developed. The desired products were obtained with high conversion and in enantiomeric excesses of 97–99% ee. Furthermore, this method has been applied in the synthesis of an N-chloroacetylated 2-cyanopyrrolidine, which represents a building block for the synthesis of Vildagliptin.

中文翻译：

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对映体纯的合成Ñ通过肟的催化脱水-酰基氨基腈，并在应用从头维格列汀的合成

一种基于对醛肟的Cu（OAc）₂催化脱水的对映异构体高度富集的N-酰基氨基腈的替代路线，该路线很容易从N-酰基l-或d -α-氨基醛中通过与羟胺缩合而获得。发达。所需的产物以高转化率和对映体过量97–99％ee获得。此外，该方法已经应用于N-氯乙酰化的2-氰基吡咯烷的合成，其代表了维格列汀的合成的基础。