Sandwich, United Kingdom
Sandwich, United Kingdom

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Bradley P.A.,Pfizer | Carroll R.J.,Research API | Lecouturier Y.C.,Pfizer | Moore R.,Research API | And 4 more authors.
Organic Process Research and Development | Year: 2010

This contribution describes the initial preparation of two potent β-3 receptor agonists 1 and 2. Subsequent scale up of these two compounds was required for further evaluation and proceeded via a common key amine intermediate 24. Synthesis of this key intermediate by way of a Ritter reaction was a vital step in the sequence. Enantioselective Noyori hydrogenation reactions gave access to the chiral epoxides necessary to make the target compounds. Chemistry was developed for the selective dehalogenation of the 2-chloropyridyl group in the presence of a sensitive isoxazole unit to provide access to 1. © 2010 American Chemical Society.


Knight C.J.,Research API | Millan D.S.,Pfizer | Moses I.B.,Research API | Robin A.A.,Research API | Selby M.D.,Pfizer
Organic Process Research and Development | Year: 2012

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. © 2012 American Chemical Society.

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