6523-63-3Relevant articles and documents
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.
, 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.
CARBOXAMIDE DERIVATIVES AS MUSCARINIC RECEPTOR ANTAGONISTS
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Page/Page column 41, (2008/06/13)
The invention relates to compounds of Formula (I) processes and intermediates for their preparation, their use as muscarinic antagonists and pharmaceutical composition containing them.