Development of a dynamic-kinetic resolution (DKR) for the synthesis of enantiomerically pure tertiary alcohols

开发用于合成对映体纯叔醇的动态动力学拆分 (DKR)

• 批准号: 418711059
• 负责人: Professor Dr. Harald Gröger
• 金额: --
• 依托单位: Arbeitsgruppe Organische Chemie I
• 依托单位国家: 德国
• 项目类别: Research Grants
• 财政年份: 2019
• 资助国家: 德国
• 起止时间: 2018-12-31 至 2023-12-31
• 项目状态: 已结题
• 来源: https://gepris.dfg.de/gepris/projekt/418711059?language=en
• 关键词: Development; dynamic; kinetic; resolution; DKR

This research project centers on the development of the first example of a dynamic kinetic resolution (DKR) of tertiary alcohols. Such a process would be of high importance for the synthesis of a range of pharmaceutically relevant intermediates. While the DKR of secondary alcohols is described in the literature, the DKR of tertiary alcohols is unknown so far. Thus, this project should find a "proof of concept" and solution for this scientific challenge. Toward this end, the following five working packages will be studied:I. Identification of suitable biocatalysts for the acylation of tertiary alcoholsII. Identification of suitable metal catalysts for the racemization of tertiary alcoholsIII. Studies on the compatibility of biocatalyst and racemization catalystIV. Development of a dynamic kinetic resolution of tertiary alcoholsV. Extension of the substrate scope and application toward the synthesis of Efavirenz® and a tribenzotriquinacene derivative

该研究项目的中心是开发叔醇的第一个动态动力学拆分（DKR）实例。这种方法对于合成一系列药学相关中间体将是非常重要的。虽然文献中描述了仲醇的DKR，但叔醇的DKR至今未知。因此，该项目应该为这一科学挑战找到“概念证明”和解决方案。为此，将研究以下五个工作包：叔醇酰化反应生物催化剂的筛选2。叔醇外消旋化反应中合适金属催化剂的鉴定III.生物催化剂与消旋催化剂相容性的研究IV.叔醇的动态动力学拆分研究V.扩大底物范围和应用，合成依法韦仑®和三苯并三喹并苯衍生物