Solution Phase Libraries by Fluorous Mixture Synthesis

第二阶段SBIR的目标是进行研究和开发，使氟技术公司。从目前的分析/示范库逐步发展到实际生产的库，其规模和规模将对制药和生物技术公司具有吸引力。一旦这种能力到位，FTI打算成为组合库合成外包市场上极具竞争力的参与者。目前估计2000年这一市场的价值为1.45亿美元，年增长率为15%。此外，该技术还将商业化用于外部使用。在成功的第一阶段工作的基础上，该赠款建议使用该公司创新的新“氟混合物合成”平台，以2-3毫克的规模合成4800 - 9600个成员的马匹辛类似物库。这项工作分为“准备阶段”和“生产阶段”，在“准备阶段”，将准备所有所需的起始材料、氟标签和多样性反应物，在“生产阶段”，将生产、纯化和分析文库。拟议的商业应用：该研究将验证FTI的氟混合物合成技术在真实的世界设置。该公司计划将这些技术用于合同库合成，并将其提供给整个社区。

The goal of the Phase II SBIR is to conduct research and development that will allow Fluorous Technologies, Inc. to ramp up from current analytical/demonstration libraries to the actual production of libraries of a size and scale that will be attractive to pharmaceutical and biotechnology companies. Once this capability is in place, FTI intends to be a highly competitive player in the outsourcing market for combinatorial library synthesis. This market is currently estimated at $145 million for 2000, with an annual growth rate of 15%. In addition, the technology will also be commercialized for external use. Building on successful Phase I work, the grant proposes the synthesis of 4,800-9,600 member library of mappicine analogs on 2-3 mg scale using the company's innovative new "fluorous mixture synthesis" platform. The work is divided into the "preparation phase", where all the needed starting materials, fluorous tags, and diversity reactants will be prepared, and the "production phase", where the library will be produced, purified and analyzed. PROPOSED COMMERCIAL APPLICATION: The research will validate FTI's fluorous mixture synthesis techniques in a real world setting. The company plans to use the techniques in- house for contract library synthesis and to make them available to the community at large.