A Method for the Alkylation of Alcohols and Amines

醇和胺的烷基化方法

• 批准号: 7282409
• 负责人: Seth B. Herzon
• 金额: $ 3.34万
• 依托单位: UNIVERSITY OF ILLINOIS AT URBANA-CHAMPAIGN
• 依托单位国家: 美国
• 财政年份: 2006
• 资助国家: 美国
• 起止时间: 2006-08-14 至 2008-04-17
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/7282409
• 关键词: Alcohols; Aldehydes; Alkaloids; Alkenes; Alkylation; Amination; Amines; Amino Alcohols; Area; Biological; Carbon; Chemicals; Chemistry; Coupling; Development; Diamines; Fellowship; Glycol; Goals; Imines; Individual; Label; Ligands; Mediating; Methods; Names; Object Attachment; Paclitaxel; Pharmaceutical Preparations; Physical condensation; Process; Research; Research Proposals; Scheme; Staging; Structure; Strychnos; Technology; Therapeutic Agents; Vancomycin; Variant; catalyst; dehydrotubifoline; programs

DESCRIPTION (provided by applicant): This goal of this research is the development of a new method for the stereocontrolled synthesis of secondary alcohols, acylic aliphatic amines, 1,2-diols, 1,2-amino alcohols, and 1,2-diamines. Such motifs are found in compounds of biological and medicinal importance, the drugs Taxol, vancomycin, and indinivar being notable examples. The method will allow for the formation of these compounds directly from primary alcohols and acylic aliphatic amines, starting materials which are abundant and widely accesible. It is envisioned that the technologies developed in this program will find use in the synthesis of natural and unnatural therapeutic agents; this will be demonstrated by the application of these methods to the total synthesis of the Strychnos alkaloid (-)-dehydrotubifoline. A portion of the research will examine the development of asymmetric C-H bond activation processes, an area of chemistry which is still largely unexplored.

描述（由申请人提供）：本研究的目标是开发一种立体控制合成仲醇、非环状脂肪胺、1，2-二醇、1，2-氨基醇和1，2-二胺的新方法。这种基序在具有生物学和医学重要性的化合物中发现，药物紫杉醇、万古霉素和茚地瓦是值得注意的例子。该方法将允许直接从伯醇和非环状脂肪族胺形成这些化合物，这些原料是丰富且广泛可获得的。据设想，该计划中开发的技术将用于天然和非天然治疗剂的合成;这将通过将这些方法应用于马钱子生物碱（-）-脱氢tubifoline的全合成来证明。部分研究将探讨不对称C-H键活化过程的发展，这是一个尚未探索的化学领域。

项目成果

Hydroaminoalkylation of unactivated olefins with dialkylamines.

• DOI: 10.1021/ja806367e
• 发表时间: 2008-11-12
• 期刊: Journal of the American Chemical Society
• 影响因子: 15
• 作者: Herzon SB;Hartwig JF
• 通讯作者: Hartwig JF