New Approaches to Site-Selective Fluorination

位点选择性氟化的新方法

• 批准号: 1465131
• 负责人: Thomas Lectka
• 金额: $ 42万
• 依托单位: Johns Hopkins University
• 依托单位国家: 美国
• 项目类别: Standard Grant
• 财政年份: 2015
• 资助国家: 美国
• 起止时间: 2015-09-01 至 2018-08-31
• 项目状态: 已结题
• 来源: https://www.nsf.gov/awardsearch/showAward?AWD_ID=1465131&HistoricalAwards=false
• 关键词: New; Approaches; Site; Selective; Fluorination

AbstractIn this project funded by the Chemical Synthesis program of the Chemistry Division, Professor Thomas Lectka of Johns Hopkins University is developing new chemical methods focused on site-selective fluorination to produce chemically interesting products not easily accessible by other means. At Johns Hopkins, Professor Lectka, supervises a research group that contains predominately undergraduates. In addition, graduate students are participants in the K-12 educational outreach program and also the Chemistry Olympiad; in a separate program offered by Hopkins called LEAD, two grad students spend time mentoring inner-city Baltimore middle school students twice a week in science and math. In summary, the P.I. plans to continue a track record of educating underrepresented minority groups (especially African-American and Hispanic undergraduates) for the foreseeable future.Operational simplicity, low catalyst loadings (where applicable), mutual compatibility, mild conditions, and broad scope are the fundamental goals. The recent, widespread interest in fluorine chemistry stems primarily from the utility of fluorinated compounds as pharmaceuticals. Nearly one quarter of the top pharmaceuticals on the market contain fluorine, placing synthetic fluorination methods, particularly those amenable to late-stage functionalization, among the most valuable warheads in the arsenal of the medicinal chemist.

在这项由化学系化学合成计划资助的项目中，约翰霍普金斯大学的Thomas Lectka教授正在开发新的化学方法，重点是位置选择性氟化，以生产其他方法不易获得的化学有趣的产品。在约翰斯·霍普金斯大学，莱特卡教授领导着一个研究小组，该小组主要由本科生组成。此外，研究生也是K-12教育推广项目和化学奥林匹克竞赛的参与者；在霍普金斯大学提供的另一个名为Lead的项目中，两名研究生每周花两次时间指导巴尔的摩市中心的中学生学习科学和数学。总而言之，在可预见的未来，P.I.计划继续教育少数族裔群体(特别是非裔美国人和西班牙裔本科生)。操作简单、催化剂负载量低(如果适用)、相互兼容、条件温和和范围广泛是基本目标。最近，人们对氟化学的广泛兴趣主要源于含氟化合物作为药物的用途。市场上近四分之一的顶级药物含有氟，这使合成氟化方法，特别是那些适合于后期功能化的方法，成为药物化学家最有价值的弹头之一。