1355533-05-9Relevant academic research and scientific papers
Development of a scaleable synthesis of a geminal dimethyl tertiary amine as an inhaled muscarinic antagonist for the treatment of COPD
Dillon, Barry R.,Roberts, Dannielle F.,Entwistle, David A.,Glossop, Paul A.,Knight, Craig J.,Laity, Daniel A.,James, Kim,Praquin, Celine F.,Strang, Ross S.,Watson, Christine A. L.
supporting information; experimental part, p. 195 - 203 (2012/06/05)
An efficient and scalable process for the synthesis of muscarinic antagonist, PF-3635659 1, is described, illustrating redesign of an analogue-targeted synthesis which contained a scale-limiting rhodium-activated C-H amination step. The final route includes a reproducible modified Bouveault reaction which has not previously been reported on a substrate of this complexity, or on such a scale with over 5 kg of the requisite gem-dimethylamine prepared via this methodology.
