Feb 122015
Here, we report a continuous flow protocol for the [3 + 2] cycloaddition of nitrones, in situ generated from oximes, into bicyclic isoxazolidines. This thermal process required very high temperatures to be efficient that were not easily reached in conventional reactors. A couple of examples are presented and in both the flow process showed a greater performance than the batch mode. The process intensification study allowed the generation of 120 g/h of a key pharmaceutical intermediate.
Large-Scale Continuous Flow Transformation of Oximes into Fused-Bicyclic Isoxazolidines: An Example of Process Intensification
see
http://pubs.acs.org/doi/abs/10.1021/op500350y
† Centro de Investigación Lilly S.A., Avda. de la Industria 30, Alcobendas-Madrid 28108, Spain
‡ Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, Indiana 46285,United States
Org. Process Res. Dev., Article ASAP
DOI: 10.1021/op500350y
Publication Date (Web): January 28, 2015
Copyright © 2015 American Chemical Society
*E-mail: rinconja@lilly.com.
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