Use of a Design of Experiments approach for the optimisation of a microwave assisted Ugi reaction.
The utility of a Design of Experiments (DoE) approach for the rapid and efficient optimisation of a microwave assisted Ugi 3cc reaction of levulinic acid is demonstrated. DoE methods have also been applied to the assessment of the reaction scope for a range of amine and isonitrile substrates. The optimal procedure developed using this approach has enabled the preparation of lactam derivatives in moderate to excellent yields (17-90%) in a reaction time of only 30 min compared to the conventional methodology which required up to 48 h.
Tye
Heather
H
Evotec OAI, 151 Milton Park, Abingdon, Oxfordshire, UK OX14 4SD. heather.tye@evotecoai.com
Whittaker
Mark
M