65144-65-2Relevant articles and documents
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.