权益分类	功能权益	普通用户	{{item.name}}会员
{{category.name}}	{{benefitItem.name}}

MAPPICINE LIBRARIES BY FLUOROUS MIXTURE SYNTHESIS

通过氟混合物合成的马匹碱文库

基本信息

批准号：
6298621
负责人：
WEI ZHANG
金额：
$ 10万
依托单位：
FLUOROUS TECHNOLOGIES, INC.
依托单位国家：
美国
项目类别：
财政年份：
2001
资助国家：
美国
起止时间：
2001-04-10 至 2001-10-09
项目状态：
已结题

来源：
https://reporter.nih.gov/project-details/6298621
关键词：
alkaloids chemical registry /resource chemical synthesis combinatorial chemistry drug discovery /isolation fluorine high performance liquid chromatography

项目摘要

DESCRIPTION: (Applicant's description) Development of a fundamental new technology for fluorous mixture synthesis is proposed. A series of new fluorous tags will be made and tested for their ability to mediate fluorous mixture synthesis of representative small organic molecules. The use of the tags and the new mixture method will be validated with the synthesis of a 100 compound library of analogs of the natural product mappicine. The mixture library synthesis will require 13 steps whereas existing fluorous parallel synthesis methods would require 130 steps. This new fluorous mixture technology will dramatically expedite the synthesis of small molecule combinatorial libraries for use in drug discovery and drug optimization research. The technology is not "disease specific" and can be applied to a broad range of biological targets in any disease area. The technology is also not "chemistry specific" and can be applied to virtually any kind of organic reaction sequence. The technology captures the advantages of mixture synthesis (fewer steps, less expense, less effort, more compounds made), but still provides pure compounds that are readily identified. PROPOSED COMMERCIAL APPLICATION: Commercial applications along two lines are envisioned. First, the company will contract with pharmaceutical and biotechnological companies to use its proprietary technologies to make libraries of new drug candidates. Second, the technology will be commercialized to provide the option of in house application for those companies who perfer not to out- source their discovery efforts.

描述：(申请人的描述)开发一项基本的新技术提出了含氟混合物的合成工艺。一系列新型氟化合物将制作标签并测试其调节氟混合物的能力代表性有机小分子的合成。标记的使用和新的混合方法将通过合成100个化合物进行验证天然产物Mappicine的类似物库。MIX图书馆合成将需要13步，而现有的氟平行合成方法需要130个步骤。这种新的氟混合物技术将极大地加快合成速度用于药物发现和药物开发的小分子组合文库优化研究。这项技术不是“疾病特效性的”，可以适用于任何疾病地区的广泛生物靶标。这个技术也不是“特定于化学的”，几乎可以应用于任何一种有机反应序列。这项技术抓住了混合物合成(步骤更少，费用更少，工作量更少，化合物更多制造)，但仍提供易于识别的纯化合物。建议的商业应用：设想了两条路线的商业应用。首先，该公司将与与制药和生物技术公司合作使用其专有技术来建立候选新药的资料库。第二，这项技术将商业化为那些不愿在以下情况下提出申请的公司提供内部申请的选择为他们的探索努力寻找来源。