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Kinetic Resolution of Oxazinones: Rational Exploration of Chemical Space through the Design of Experiments |
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| Authors: | Polyssena Renzi Christel Kronig Dr Armando Carlone Dr Serap Eröksüz Prof Dr Albrecht Berkessel Dr Marco Bella |
| Affiliation: | 1. Department of Chemistry, “Sapienza” University of Roma and Istituto di Chimica Biomolecolare del CNR, P.le Aldo Moro 5, 00185 Roma (Italy);2. Chirotech Technology Centre, Dr. Reddy's Laboratories (EU) Ltd 410, Cambridge Science Park, Milton Road Cambridge CB4 0PE (UK);3. Department für Chemie, Organische Chemie, Universit?t zu K?ln, Greinstra?e 4, 50939 K?ln (Germany) |
| Abstract: | The organocatalytic kinetic resolution of 4‐substituted oxazinones has been optimised (selectivity factor S up to 98, chiral oxazinone ee values up to 99.6 % ( 1 a – g ) and product ee values up to 90 % ( 3 a – g )) in a rational way by applying the Design of Experiments (DoE) approach. |
| Keywords: | design of experiments kinetic resolution organocatalysis squaramides thioureas |
