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...