Si-ROMP Hybrid Reagent/Scavengers for High Throughput Chemistry

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DESCRIPTION (provided by applicant): This Fast Track Small Business Technology Transfer study between Materia, Inc. and the University of Kansas intends to build upon successes of our current STTR Phase II grant (R41GM076765-02) which expires on March 31, 2011. This proposal is a collaborative effort between the University of Kansas and Materia, Inc. in Pasadena, CA that aims to develop and scale-up Si-ROMP hybrid reagents/scavengers and optimize the process for their commercialization. More specifically, Phase I will focus on three key areas: (1) Generation of an array of Si-ROMP reagent/scavengers from existing and new norbornenyl-functionalized monomers utilizing surface-initiated ROM polymerization off SiO2 surfaces, with a Phase I milestone goal to synthesize six Si- ROMP reagents: Si-OBAC, Si-ODCT, Si-OTPP, Si-OTP, Si-OACC and Si-OBP, (2) Utilization of the developed Si-ROMP hybrid materials in flow-through technology for facile and purification-free protocols in high throughput methods, with another Phase I milestone goal demonstrating utilization of Si-ROMP hybrid materials in continuous-flow protocols. The Phase II goals are (3) process development and scale-up of Si-ROMP reagents and scavengers including key beta-testing of Si-ROMP reagents and scavengers by industrial and non-profit organization/collaborators, (4) continued generation of surface-immobilized reagent/scavengers from existing and new norbornenyl-functionalized monomers utilizing surface-initiated ROM polymerization (Aim #1 in Phase 1), (5) continued utilization of the developed Si-ROMP hybrid materials in flow-through technology for facile and purification-free protocols in high throughput methods (Aim #2 in Phase 1), and (6) utilization of Nb-tagged Si-particles to sequester Nb-tagged reagents/scavengers in facile and purification-free protocols and investigation into recycling of spent Si-ROMP cartridges. Application of soluble versions of ROMP reagents for drug-discovery has been demonstrated through a number of studies in our currently funded Phase II as well as in recent publications. We are well positioned to meet the challenging technical aspects of the proposed Fast Track program through teaming of scientists at Materia, Inc. and the University of Kansas. Moreover, Materia's technology platforms, its business development unit, and large scale manufacturing facilities will facilitate the planned transition of the developed technologies out of the laboratory and into the commercial realm. Materia has developed an extensive strategic alliance network to leverage its technical and business resources and accelerate downstream product development. Extensive resources in the Principal Investigator's laboratory, the NIH Center in Chemical Methodologies for Library Development at the University of Kansas (KU-CMLD), and at Materia, Inc. will be utilized toward product development and extensive beta testing of all products offered for commercialization.