65144-65-2Relevant academic research and scientific papers
Kilogram-scale synthesis of an inhaled corticosteroid
Knight, Craig J.,Millan, David S.,Moses, Ian B.,Robin, Aurelie A.,Selby, Matthew D.
experimental part, p. 697 - 703 (2012/08/07)
The development and implementation of a safe and scalable process for the manufacture of corticosteroid PF-4714224 (1) is described. Initial routes used to synthesise analogues from this series directly from fluocinolone acetonide (2) were unsuitable for large-scale use. Key aspects of the route are the efficient and simple method for the preparation of the steroid tetraol (6), acetal formation by reaction of the tetraol with a bisulphite adduct (12), and isolation of the product by sequential recrystallisations.
NOVEL GLUCOCORTICOID RECEPTOR AGONISTS
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Page/Page column 37, (2009/07/03)
This invention relates to novel glucocorticoid receptor agonists of formula (I) and to processes and intermediates for their preparation. The present invention also relates to pharmaceutical compositions containing these compounds, to their combination with one or more other therapeutic agents, as well as to their use for the treatment of a number of inflammatory and allergic diseases, disorders and conditions.
