The synthesis of two potent β-3 adrenergic receptor agonists

…, P Noeureuil, B Patel, J Snow, S Wheeler

Index: Bradley, Paul A.; Lecouturier, Yann C.; Noeureuil, Pierre; Patel, Bhairavi; Wheeler, Simon; Carroll, Robert J.; Moore, Robert; Snow, Jonathan Organic Process Research and Development, 2010 , vol. 14, # 6 p. 1326 - 1336

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Citation Number: 20

Abstract

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 ...