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

可回收磁性 Co/C 混合 ROMP 试剂、清除剂和配体

• 批准号: 8917321
• 负责人: PAUL R. HANSON
• 金额: $ 49.47万
• 依托单位: MATERIA, INC.
• 依托单位国家: 美国
• 财政年份: 2014
• 资助国家: 美国
• 起止时间: 2014-09-01 至 2017-08-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/8917321
• 关键词: Address; Area; Automobile Driving; Businesses; Chemicals; Collaborations; Development; Foundations; Generations; Goals; Grant; Health; Human; Hybrids; Hydrochloride Salt; Immobilization; Institutes; Kansas; Laboratories; Letters; Libraries; Ligands; Magnetic nanoparticles; Magnetism; Metals; Methodology; Methods; Mission; Molecular; Natural regeneration; Pharmacologic Substance; Phase; Poaceae; Positioning Attribute; Process; Production; Property; Protocols documentation; Reaction; Reagent; Resources; Seminal; Small Business Technology Transfer Research; Solid; Succinimides; Surface; Swelling; Switzerland; Technology; Technology Transfer; United States National Institutes of Health; Universities; biological systems; catalyst; chemical synthesis; commercialization; drug discovery; improved; meetings; monoamine; nanoparticle; new technology; particle; physical property; polymerization; process optimization; professor; pyridine; reagent testing; scale up; small molecule; small molecule libraries; success; tool; triphenylphosphine

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.

描述（由申请人提供）：Materia，Inc.位于加州帕萨迪纳市和堪萨斯大学打算在我们目前的第二阶段快速通道STTR资助（1 R42 GM 097896 -03）的成功基础上再接再厉，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混合ROMP配体/试剂/清除剂的开发”的快速通道提交奠定了坚实的基础。该提案旨在开发、优化和扩大可回收的磁性Co/C杂合ROMP配体/试剂/清除剂，并简化其商业化的过程。更具体地说，第一阶段将侧重于两个关键领域：即，（1）利用表面引发的ROM聚合开发和产生多克量的五种可再循环的、磁性的、高负载的Co/C混合ROMP配体/试剂/清除剂，其中阶段I里程碑目标是合成和多克规模放大五种试剂，即Co/C-OTPP、Co/C-OOAS、Co/C-OPC、Co/COMam和Co/COPY，和（2）磁性Co/C杂化ROMP试剂在合成转化中的利用，用于促进小分子的合成，在平行合成和螯合方案中的应用。第二阶段的目标有三个方面，包括：（3）利用表面引发的ROM聚合，开发固定在Co/C磁性NP上的高负载、ROMP衍生的寡聚配体/催化剂、试剂和清除剂的阵列，（4）用于扩大可再循环的、磁性的、高负载Co/C-ROMP杂合试剂的工艺优化，和（5）这些混合磁性试剂在合成转化中的利用，用于促进小分子的合成、在平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方面的专业知识，能够很好地应对这一提议的挑战（KU和Materia Inc.），与里根斯堡大学的奥利弗雷泽教授、瑞士苏黎世的瑞士联邦理工学院（ETHZ）的罗伯特·格拉斯博士（Dr. Robert Grass）合作的Co-C纳米颗粒技术，以及在堪萨斯大学的化学方法学和库开发中心（KU-CMLD）内使用ROMP试剂生产化学库。Materia，Inc.的核心技术和专业知识增强了这些努力。用于工艺优化和放大合成。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。