Organic Process Research and Development p. 1521 - 1527 (2017)
Update date:2022-08-10
Topics:
Rommelmann, Philipp
Betke, Tobias
Gr?ger, Harald
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.
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