Solution Phase Libraries by Fluorous Mixture Synthesis

含氟混合物合成溶液相库

• 批准号: 6485131
• 负责人: WEI ZHANG
• 金额: $ 96.02万
• 依托单位: FLUOROUS TECHNOLOGIES, INC.
• 依托单位国家: 美国
• 财政年份: 2001
• 资助国家: 美国
• 起止时间: 2001-04-10 至 2004-03-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6485131
• 关键词: alkaloids; chemical registry /resource; chemical synthesis; combinatorial chemistry; drug discovery /isolation; fluorine; high performance liquid chromatography; quinoline

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.

第二阶段SBIR的目的是进行研究和开发，以使富有的Technologies，Inc。从当前的分析/示范库增加到大小和规模的实际生产，这对制药和生物技术公司都有吸引力。一旦实现此功能，FTI打算成为组合图书馆综合外包市场中竞争激烈的参与者。该市场目前估计为2000年的1.45亿美元，年增长率为15％。此外，该技术还将商业化以供外部使用。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型“氟混合物合成”平台合成2-3毫克比例的Mappicine类似物的4,800-9,600成员库。该作品分为“制备阶段”，其中将准备所有所需的起始材料，易流的标签和多样性反应物，以及将生成，纯化和分析库的“生产阶段”。拟议的商业应用：该研究将在现实世界中验证FTI荧光混合物合成技术。该公司计划使用这些技术来进行合同图书馆合成，并将其提供给社区的整个社区。

项目成果

Fluorous synthesis of hydantoins and thiohydantoins.

• DOI: 10.1021/ol034854a
• 发表时间: 2003-07
• 期刊: Organic letters
• 影响因子: 5.2
• 作者: Wei Zhang-;Yimin Lu

Microwave-Enhanced Fluorous Synthesis.

微波增强氟合成。

• 发表时间: 2005
• 期刊: Chimica oggi
• 作者: Zhang,Wei

Microwave-Enhanced High-Speed Fluorous Synthesis.

微波增强高速氟合成。

• DOI: 10.1007/128_045
• 发表时间: 2006
• 期刊: Topics in current chemistry
• 影响因子: 8.6
• 作者: Zhang,Wei

Combination of microwave reactions with fluorous separations in the palladium-catalyzed synthesis of aryl sulfides.

钯催化芳基硫醚合成中微波反应与氟分离的结合。

• DOI: 10.1023/b:modi.0000006825.12186.5f
• 发表时间: 2003
• 期刊: Molecular diversity
• 影响因子: 3.8
• 作者: Zhang,Wei;Lu,Yimin;Chen,ChristineHiu-Tung
• 通讯作者: Chen,ChristineHiu-Tung

Fluorous Synthesis of Hydantoin-, Piperazinedione-, and Benzodiazepinedione-Fused Tricyclic and Tetracyclic Ring Systems.

• DOI: 10.1002/ejoc.200600077
• 发表时间: 2006-05
• 期刊: European journal of organic chemistry
• 影响因子: 2.8
• 作者: Wei Zhang-;Yimin Lu;C. Chen;D. Curran;S. Geib