Development of a One-Pot Procedure for the Synthesis of Cyclopropylamines

环丙胺合成一锅法的开发

• 批准号: 521725-2017
• 负责人: Rousseaux, Sophie
• 金额: $ 1.82万
• 依托单位: University of Toronto
• 依托单位国家: 加拿大
• 项目类别: Engage Grants Program
• 财政年份: 2017
• 资助国家: 加拿大
• 起止时间: 2017-01-01 至 2018-12-31
• 项目状态: 已结题
• 来源: https://www.nserc-crsng.gc.ca/ase-oro/Details-Detailles_eng.asp?id=640174
• 关键词: Development; Pot; Procedure; Synthesis; Cyclopropylamines

The cyclopropylamine motif is found in numerous pharmaceuticals and agrochemicals. Therefore, methods toprepare these compounds are highly desirable. This Engage Grant will explore a new method to preparecyclopropylamines from readily accessible starting materials based on recent results obtained by the Rousseauxgroup in this area.Inception Sciences Canada has found that introduction of a cyclopropylamine motif in one of their smallmolecule therapeutics is beneficial for overall potency while also leading to desirable metabolic properties. Themethod developed by the Rousseaux group in the context of this Engage Grant will enable Inception Sciencesto rapidly construct a large library of cyclopropylamines and facilitate the synthesis of analogs.

环丙胺基序存在于许多药物和农用化学品中。因此，非常需要制备这些化合物的方法。根据Rousseauxgroup在这一领域的最新研究成果，该Engage Grant将探索一种新的方法，从容易获得的起始材料中合成环丙胺。Inception Sciences Canada发现，在其小分子治疗药物中引入环丙胺基序有利于整体效力，同时也导致理想的代谢特性。Rousseaux小组在该Engage Grant的背景下开发的方法将使Inception Sciences能够快速构建一个大型的环丙胺库并促进类似物的合成。