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

描述(由申请人提供)：这项位于加利福尼亚州帕萨迪纳市的Materia，Inc.与堪萨斯大学之间的快速通道小型企业技术转让研究旨在建立在我们目前第二阶段快速通道技术转让资助(1R42GM097896-03)成功的基础上，该资助将于2014年3月30日结束。初步结果为这份题为《可回收磁性Co/C杂化ROMP配体/试剂/清道夫的发展》的快速报告奠定了坚实的基础。这项提议旨在开发、优化和放大可回收的磁性Co/C杂化ROMP配体/试剂/清道夫，并简化其商业化进程。更具体地说，第一阶段将集中在两个关键领域：即(1)利用表面引发的只读存储器聚合开发和产生多克数量的可回收、磁性、高负载的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合成和放大五种试剂，即Co/C-OTPP、Co/C-OOAS、Co/C-OPC、Co/C OMAM和Co/C OPY，以及(2)利用磁性Co/C杂化ROMP试剂进行合成转化以促进小分子的合成，在并行合成和隔离协议中的应用。第二阶段的目标有三个，包括：(3)利用表面引发的只读存储器聚合，开发一系列固定在Co/C磁性纳米粒子上的高负载、由ROMP衍生的低聚配体/催化剂、试剂和清除剂，(4)优化可回收、磁性、高负载Co/C-ROMP杂化试剂的放大工艺，以及(5)利用这些混合磁性试剂进行合成转化，以促进小分子的合成，在并行合成和自动化技术中的应用。我们在使用ROMP技术生产可溶性和硅固定化试剂(KU和Materia Inc.)、与雷根斯堡大学的Oliver Reiser教授、瑞士苏黎世联邦理工学院(ETHZ)的Robert Grass博士开展的Co-C纳米粒子技术合作以及在堪萨斯大学化学方法和图书馆开发中心(KU-CMLD)内使用ROMP试剂生产化学图书馆(KU-CMLD)方面拥有专业知识，能够很好地应对这项提议的挑战。在这些努力的基础上，增加了MATRIA公司用于工艺优化和放大合成的核心技术和专业知识。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贝塔测试。如果成功，这些磁性试剂将代表一种新的商业化绿色技术，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.