Improved stereoselectivity in the heterogeneous catalytic synthesis of enalapril obtained through multidimensional screening

A multidimensional screening of catalysts and additives led to the discovery of improved conditions for the diastereoselective reductive amination which produces enalapril. Additives acetic acid and potassium fluoride, which in isolation are detrimental, work together to improve the SSS : RSS select...

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Bibliographic Details
Published in:Tetrahedron letters 1999-01, Vol.40 (5), p.831-834
Main Authors: Huffman, Mark A., Reider, Paul J.
Format: Article
Language:English
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Summary:A multidimensional screening of catalysts and additives led to the discovery of improved conditions for the diastereoselective reductive amination which produces enalapril. Additives acetic acid and potassium fluoride, which in isolation are detrimental, work together to improve the SSS : RSS selectivity with Ra-Ni in ethanol to 17 : 1 from 11 : 1. A unique combination of heterogeneous catalyst and 2 additives raised the SSS:RSS selectivity to 17:1
ISSN:0040-4039
1873-3581
DOI:10.1016/S0040-4039(98)02590-8