1251957-77-3Relevant articles and documents
The synthesis of two potent β-3 adrenergic receptor agonists
Bradley, Paul A.,Lecouturier, Yann C.,Noeureuil, Pierre,Patel, Bhairavi,Wheeler, Simon,Carroll, Robert J.,Moore, Robert,Snow, Jonathan
, p. 1326 - 1336 (2011/09/20)
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.
