Optimization of the synthesis of a key intermediate for the preparation of glucocorticoids

Steroids
Romain JouveKhalil Bennis

Abstract

A short and efficient synthesis, based on a one-step double elimination, of a key intermediate in the synthesis of various glucocorticosteroids has been developed. This method can be carried out on large scale for further industrial applications. The synthesis allowed us to identify a novel prednisolone derivative 10 and its anti-inflammatory activity was determined in an in vivo model of inflammation. In order to understand the regioselectivity of the double elimination under various conditions, mechanistic studies were undertaken and confirmed the experimental results. We also propose a mechanism for the formation of the new steroid 10 studied by molecular modeling.

References

Jul 8, 2010·The Journal of Gene Medicine·Carol KilkennyUNKNOWN NC3Rs Reporting Guidelines Working Group
Jul 24, 2010·British Journal of Pharmacology·J C McGrathC L Wainwright
May 1, 2006·Journal of Chemical Theory and Computation·Thom VrevenMichael J Frisch

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