Development of a Commercial Flow Barbier Process for a Pharmaceutical Intermediate
Contributor(s):: Braden, Timothy M., Johnson, Martin D., Kopach, Michael E., Groh, Jennifer McClary, Spencer, Richard D., Lewis, Jeffrey, Heller, Michael R., Schafer, John P., Adler, Jonathan J.
A flow Barbier process was developed to produce a key intermediate in the edivoxetine·HCl registered sequence. The control strategy was developed based on a critical understanding of integrated parameters and design space requirements for a continuous stirred tank reactor (CSTR) process. In this...
Continuous GMP Manufacturing for Grignard Reagent/Zincate Synthesis and Negishi Coupling Reaction
Contributor(s):: Calvin, Joel R., Boyse, Raymond, Braden, Timothy M., Brewer, Alison C, Changi, Shujauddin, Harrold, Donal, Johnson, Martin, Kerr, Mark S., Lambertus, Gordon R., Luciani, Carla V., May, Scott A., Moloney, Harold, Murphy, John D., Roberts, Jeffrey C., Schafer, John P., Spencer, Richard D., Webster, Luke P.
A synthetic route to API was designed containing a Negishi cross-coupling reaction, where the zincate reagent was generated by transmetalation of a Grignard reagent. In order to manage the poor stability of the Grignard reagent, as well as safety concerns, the chemistry was developed as a flow...