通过化物转移策略启用形式 [5 + 1] 和 [5 + 2] 循环的N-异环的可控合成
Ying Dong1, Fangzhi Hu1, Huixin Wu1
1College of Chemistry and Pharmaceutical Sciences, Qingdao Agricultural University, Changcheng Rd. #700, Qingdao 266109, P. R. China.
Organic letters
|December 28, 2023
概括
一种新的布伦斯特德酸控制合成使得复杂的印度融合的四氨基和印度融合的班扎泽平能够产生. 这种方法利用化物转移反应进行高效循环,产生前所未有的五环结构.
科学领域:
- 有机合成 有机合成
- 药用化学 医学化学
- 异环化学 异环化学
背景情况:
- 对复杂的异环化合物的高效合成方法的开发对于药物发现至关重要.
- 现有的合成印度和印度融合系统的方法往往涉及多个步骤和恶劣的条件.
- 需要新的循环化策略来访问各种分子架构.
研究的目的:
- 开发一种布伦斯特德酸控制的可切换合成,用于合印林的四基诺林和合印尔的班扎泽平.
- 探索化物转移启用形式 [5 + 1] 和 [5 + 2] 循环反应的实用性.
- 通过级联过程访问前所未有的五环混合结构.
主要方法:
- 作为起始材料使用的醇和N-基o-aminobenzoketones.
- 采用布伦斯特酸催化剂来控制可切换的合成途径.
- 杆化化物转移启用正式的 [5 + 1] 和 [5 + 2] 循环反应,包括一个级联凝结/化物转移/除气-循环/脱乙/核添加过程.
主要成果:
- 成功合成了印度融合的四基诺林和印度融合的benzazepines.
- 取得了前所未有的印度林, furanone 和 tetrahydroquinoline 杂交的五环制品.
- 证明了第一个报告的化物转移涉及的 [5 + 2] 循环化,用于直接构建合印的泽.
结论:
- 开发的布伦斯特德酸控制方法提供了一条有效的途径,以获得有价值的异环基架.
- 这种新型的级联反应为复杂的五环结构提供了访问权限,在药物化学中具有潜在的应用.
- 这项工作扩大了合成工具箱,用于构建基于醇的化环系统.
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