New Synthetic Methods Useful for Chemotherapeutics

可用于化疗的新合成方法

• 批准号: 6677985
• 负责人: Peter A. Beak
• 金额: $ 22.7万
• 依托单位: UNIVERSITY OF ILLINOIS AT URBANA-CHAMPAIGN
• 依托单位国家: 美国
• 财政年份: 1976
• 资助国家: 美国
• 起止时间: 1976-08-01 至 2005-07-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6677985
• 关键词: alkaloids; chemical bond; chemical reaction; drug design /synthesis /production; method development; stereochemistry

DESCRIPTION (provided by applicant): The general goal of the proposed work is to develop reactions discovered in my laboratory which can provide new approaches for asymmetric syntheses of biologically active compounds. Prototypical reactions for the creation of asymmetric carbon-carbon bonds by lithiation substitution sequences in the presence of a chiral ligand will be investigated. The focus of the application is on elaboration of N-Boc amines, which have been shown in our previous work to provide useful asymmetric synthetic equivalents. The reactions sequences to be studied have the potential for providing a strategic approach for asymmetric syntheses. The methodology and fundamental understanding to be provided should be of such clear advantage that synthetic schemes will be designed around this methodology. The proposed work provides convenient, efficient, asymmetric syntheses which would be useful for the preparation of chemotherapeutic agents on the discovery, development, and manufacturing scale.

描述（由申请人提供）：拟议工作的一般目标是开发我的实验室中发现的反应，该反应可以为生物活性化合物的不对称合成提供新的方法。将研究在存在手性配体的情况下通过晶格取代序列创建不对称碳碳键的典型反应。该应用的重点是详细说明N-BOC胺，这在我们以前的工作中已显示出有用的不对称合成等效物。 要研究的反应序列具有为不对称合成提供战略方法的潜力。所提供的方法和基本理解应该具有如此明显的优势，以至于围绕该方法设计了合成方案。拟议的工作提供了方便，高效，不对称的合成，这些合成对于在发现，开发和制造量表上制备化学治疗剂很有用。