The development of an enantioselective enamine-catalysed addition of masked acetaldehyde to nitroalkenes via a rational approach helped to move away from the use of chloroform. The presented research allows the use of water as a reaction medium, therefore improving the industrial relevance of a protocol to access very important pharmaceutical intermediates. Critical to the success is the use of chemometrics-assisted ‘Design of Experiments’ (DoE) optimisation during the development of the presented new synthetic approach, which allows to investigate the chemical space in a rational way.

DoE‐driven development of an organocatalytic enantioselective addition of acetaldehyde to nitrostyrenes in water

Nori, Valeria;Sinibaldi, Arianna;Giorgianni, Giuliana;Pesciaioli, Fabio;Di Donato, Francesca;Cocco, Emanuele;Biancolillo, Alessandra;Carlone, Armando
Conceptualization
2022

Abstract

The development of an enantioselective enamine-catalysed addition of masked acetaldehyde to nitroalkenes via a rational approach helped to move away from the use of chloroform. The presented research allows the use of water as a reaction medium, therefore improving the industrial relevance of a protocol to access very important pharmaceutical intermediates. Critical to the success is the use of chemometrics-assisted ‘Design of Experiments’ (DoE) optimisation during the development of the presented new synthetic approach, which allows to investigate the chemical space in a rational way.
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11697/181152
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