乌尔曼型N-,S-,和O-Arylation使用一个明确的7-Azaindole-N-oxide (7-AINO) 基铜催化剂:药物合成的范围和应用
Vishal Talukdar1, Krishanu Mondal1, Pallabi Halder1
1Department of Chemistry and Chemical Biology, Indian Institute of Technology (Indian School of Mines), Dhanbad 826004, India.
The Journal of organic chemistry
|May 22, 2024
概括
一种新型的铜 (II) -7-阿扎醇-N-氧化物催化剂有效地促进了乌尔曼型合反应. 这种具有成本效益的催化剂可实现选择性和异,促进复杂药物分子的合成.
科学领域:
- 催化剂是一种催化剂.
- 有机合成 有机合成
- 药用化学 医学化学
背景情况:
- 乌尔曼型合反应对于C-N,C-S和C-O键的形成至关重要.
- 开发高效,稳定和具有成本效益的催化剂对于更广泛的应用是必不可少的.
- 基于铜的催化剂因其可访问性和反应性而被广泛用于合反应.
研究的目的:
- 为乌尔曼型合反应开发一种强大且稳定的铜 (II) 催化剂.
- 为了研究催化剂在各种核友的化和异化中的效率.
- 为了证明催化剂在合成药物相关分子中的实用性.
主要方法:
- 基于铜(II) -7-阿扎英多尔-N-氧化物的催化剂 [Cu2 ((7-AINO)) 4]的合成和表征.
- 评估催化剂的性能在乌尔曼型合反应与各种N,S和O核友的反应.
- 评估化学和区域选择性,功能组耐受性,以及在药物合成中的应用.
主要成果:
- 空气稳定的铜II-7-azaindole-N-氧化物催化剂 (CuII-7-AINO) 已成功制备并证明了高效率.
- 催化剂促进了醇,氨醇,醇和醇的化和异化,具有广泛的功能组兼容性.
- 观察到 -NH和 -SH位点在 -NH2位点上的选择性合,增强了它的多功能性.
- 该协议成功地用于合成Epirizole类似物Nilotinib和Vortioxetine.
结论:
- 开发的Cu (II) -7-AINO催化剂为乌尔曼型合反应提供了具有成本效益和高效的解决方案.
- 催化剂的化学和区域选择性使其对复杂分子合成具有价值.
- 这种方法为合成重要的药物化合物提供了可行的途径.
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