Recyclable Magnetic Co/C Hybrid ROMP Reagents, Scavengers and Ligands

描述（由申请人提供）：加州帕萨迪纳市Materia， Inc.和堪萨斯大学之间的快速通道小企业技术转移研究旨在建立在我们目前的二期快速通道str资助（1R42GM097896-03）的成功基础上，该资助将于2014年3月30日结束。初步结果为该快速通道提交的题为“可回收磁性Co/C混合ROMP配体/试剂/清除剂的开发”奠定了坚实的基础。该提案旨在开发、优化和扩大可回收的磁性Co/C混合ROMP配体/试剂/清除剂，并简化其商业化过程。更具体地说，第一阶段将侧重于两个关键领域：即：(1)利用表面引发ROM聚合开发和生成多克数量的5种可回收的、磁性的、高负荷的Co/C杂化ROMP配体/试剂/清除剂，其中第一阶段的里程碑目标是Co/C- otpp、Co/C- ooas、Co/C- opc、Co/C OMam和Co/C OPy 5种试剂的合成和多克规模放大，以及(2)利用磁性Co/C杂化ROMP试剂进行合成转化，促进小分子的合成。平行合成和封存协议中的应用。第二阶段的目标有三个方面，包括：(3)利用表面引发ROM聚合，开发一系列高负载、ROM衍生的低聚配体/催化剂、试剂和清除剂，固定在Co/C磁性NPs上；(4)优化可回收、高负载、磁性Co/C-ROM杂化试剂的生产工艺；(5)利用这些杂化磁性试剂进行合成转化，以促进小分子的合成，并在平行合成和自动化技术中应用。我们在利用ROMP技术生产可溶性和硅固定化试剂（KU和Materia Inc.）方面的专业知识，以及与雷根斯堡大学的Oliver Reiser教授、瑞士联邦理工学院（ETHZ）的Robert Grass博士合作的Co-C纳米颗粒技术，已经做好了迎接这一提议的挑战的准备。以及在堪萨斯大学化学方法和图书馆发展中心（KU-CMLD）使用ROMP试剂生产化学文库。这些努力与Materia公司的核心技术和专业知识相结合，以优化工艺和扩大合成规模。此外，KU-CMLD和制药公司内部的协会将允许在药物发现和商品化学平台内对试剂进行beta测试。如果成功，这些磁性试剂将代表一种新的绿色商业化技术，有助于以可持续的方式简化化学实体的合成。

DESCRIPTION (provided by applicant): 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.