This Fast Track Small Business Technology Transfer study between Materia, Inc. in Pasadena, CA and the University of Kansas intends to build upon successes of our current Phase II Fast Track STTR grant (1R42GM097896-03) which ends on March 30, 2014. Preliminary results serve as a solid foundation for this Fast Track submission entitled Development of Recyclable Magnetic Co/C Hybrid ROMP Ligands/Reagents/Scavengers. This proposal aims to develop, optimize and scale-up recyclable magnetic Co/C hybrid ROMP ligands/reagents/scavengers and streamline the process for their commercialization. More specifically, Phase I will focus on two key areas: namely, (1) the development and generation of multi-gram quantities of five recyclable, magnetic, high-load Co/C hybrid ROMP ligands/reagents/scavengers utilizing surface-initiated ROM polymerization, where the Phase I Milestone Goal is the synthesis and multi-gram scale-up of five reagents, namely Co/C-OTPP, Co/C-OOAS, Co/C-OPC, Co/C OMam and Co/C OPy, and (2) utilization of magnetic Co/C hybrid ROMP reagents in synthetic transformations for the facilitated synthesis of small molecules, applications in parallel synthesis and sequestration protocols. The Phase II goals are threefold, and include: (3) the development of an array of high-load, ROMP-derived oligomeric ligands/catalysts, reagents and scavengers immobilized on Co/C magnetic NPs utilizing surface-initiated ROM polymerization, (4) process optimization for scale-up of recyclable, magnetic, high-load Co/C-ROMP hybrid reagents, and (5) utilization of these hybrid magnetic reagents in synthetic transformations for the facilitated synthesis of small molecules, applications in parallel synthesis and automated technologies. We are well-positioned to meet the challenges of this proposal with expertise in the use of ROMP technologies for the production of soluble and Si-immobilized reagents (KU and Materia Inc.), a Co-C nanoparticle technology collaboration with Professor Oliver Reiser at the University of Regensburg, Dr. Robert Grass at the Swiss Federal Institute of Technology in Zurich (ETHZ), Switzerland, and the use of ROMP reagents for production of chemical libraries within the Center for Chemical Methodologies and Library Development at The University of Kansas (KU-CMLD). These efforts are augmented with the core technologies and expertise within Materia, Inc. for process optimization and scale-up synthesis. Moreover, associations within the KU-CMLD and pharmaceutical companies will allow for beta testing of the reagents within drug discovery and commodity chemical platforms. If successful, these magnetic reagents will represent a new green technology for commercialization that will aid in streamlining the synthesis of chemical entities in a sustainable manner.
This project entitled Recyclable, Magnetic Co/C-Hybrid ROMP Ligands/Reagent/Scavengers aims for the production and commercialization of high-load, recyclable magnetic Co/C-Hybrid ROMP ligands, reagents and scavengers for the facilitated synthesis of small molecules, applications in parallel synthesis and automated technologies to aid in modern drug discovery efforts.
| Faisal, Saqib; Zang, Qin; Maity, Pradip K et al. (2017) Development and Application of a Recyclable High-Load Magnetic Co/C Hybrid ROMP-Derived Benzenesulfonyl Chloride Reagent and Utility of Corresponding Analogues. Org Lett 19:2274-2277 |
