Novel Catalyst Systems

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DESCRIPTION (provided by applicant): Transition metal catalysts are widely used in the pharmaceutical industry for the production of active ingredients, precursors and new drug candidates. These products must be very pure, often requiring labor and energy intensive separation processes, to achieve the required purity levels. Of special concern in the present context is to avoid contaminating the product with the transition metal catalyst used during its synthesis. The above references are far from an exhaustive list but suggest the breadth and importance of the chemistry available from palladium catalysts. Palladium catalyzed reactions are ubiquitous in pharmaceutical process chemistry. Many synthetic processes rely on both heterogeneous and homogeneous catalysis. However, Pd is highly toxic, and the allowable level of palladium in an active pharmaceutical ingredient (API) is highly regulated, and must be less than 5 ppm (oral) or 0.5 ppm (parenteral). Accordingly, there is considerable interest in the development of new technologies that will ameliorate the problem of metal contamination in Pd- catalyzed processes. A variety of scavenger and filtering methods are used for removing palladium from APIs. Palladium removal essentially adds an extra step to a synthesis, and is consequently costly in terms of time and money. Although palladium catalysis is the major focus of this proposal, other metal species are also of interest. Compact Membrane Systems, Inc. (CMS) proposes a new catalyst system that provides the needed catalytic reactivity as described above but eliminates the extra steps associated with reducing/eliminating contamination. In Phase I CMS will fabricate palladium system, demonstrate its catalytic capability and determine contamination level in produce. Contingencies are included and overall economic evaluation is included. PUBLIC HEALTH RELEVANCE: It is proposed to eliminate the problem of leaching of transition metal catalysts into pharmaceutical process streams, which can contaminate the product and result in loss of costly catalyst materials. Combining fluorous technology with membranes we further enhance the ability to separate metal and other components from organic species. Successful implementation of this technology should result in higher purity, lower cost products.