Kilogram-Scale Synthesis of an Inhaled Corticosteroid

Autor:	Matthew D. Selby, Aurelie A. Robin, Craig J. Knight, David S. Millan, Ian B. Moses
Rok vydání:	2012
Předmět:	medicine.drug_class medicine.medical_treatment Organic Chemistry Acetal Adduct Steroid chemistry.chemical_compound chemistry Fluocinolone acetonide medicine Organic chemistry Corticosteroid Physical and Theoretical Chemistry medicine.drug
Zdroj:	Organic Process Research & Development. 16:697-703
ISSN:	1520-586X 1083-6160
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::bb68d854c69797caca4c82fa87d14081 https://doi.org/10.1021/op200257g Zobrazit plný text záznamu