Development of an enabling route to PF-00610355: a novel inhaled β2-adrenoreceptor agonist

PD de Koning, IR Gladwell, IB Moses…

Index: De Koning, Pieter D.; Gladwell, Iain R.; Moses, Ian B.; Panesar, Maninder S.; Pettman, Alan J.; Thomson, Nicholas M. Organic Process Research and Development, 2011 , vol. 15, # 6 p. 1247 - 1255

Full Text: HTML

Citation Number: 5

Abstract

The initial route used to prepare PF-00610355 (8) for early clinical development is described. Through careful choice of solvent, an efficient, telescoped route to carboxylic acid 23 was developed, affording this late-stage intermediate in 80% yield over 4 steps. Deprotection of 23 to give sodium salt 24a and coupling with amine 6· HCl afforded the desired API. Effective synthetic routes to two of the starting materials, chiral bromide 1 and ...