4-CF3-1,2,3-Triazoles的铜催化合成:通过点击反应的有效和简单的方法
Tinghong Tang1, Cuiting Chen1, Xin Fu1
1Key Laboratory of Tropical Medicinal Resource Chemistry of Ministry of Education, College of Chemistry and Chemical Engineering, Hainan Normal University, Haikou 571158, China.
Molecules (Basel, Switzerland)
|March 28, 2024
概括
这项研究引入了一种点击反应,用于合成三甲基替代的1,2,3-triazoles. 该方法使用易于获得的前体和铜催化剂,用于高产量生产这些有价值的化学基因.
科学领域:
- 有机化学 有机化学
- 药用化学 医学化学
- 材料科学 材料科学 材料科学
背景情况:
- 1,2,3-三醇是重要的异环化合物,具有多种应用.
- 加入三甲基组可以增强有机分子的特性.
- 三甲基化异环的高效合成仍然是一个关键的挑战.
研究的目的:
- 开发一种区域选择性点击反应,用于合成1-置换-4-三甲基-1,2,3-三醇.
- 为合成利用易于获得和稳定的起始材料.
- 建立适用于广泛的亚齐德的多功能和高收益的协议.
主要方法:
- 在2-bromo-3,3,3-trifluoropropene (BTP) 中使用1,8-diazabicyclo[5.4.0]undec-7-ene (DBU) 在位生成3,3,3-trifloropropyne (TFP).
- 铜(I) 化物 (CuI) 和1,10-Phenanthroline (Phen) 催化在原位生成的TFP和各种有机亚酸盐之间的循环添加反应.
- 格拉姆尺度合成来证明协议的可扩展性.
主要成果:
- 点击反应以高的区域选择性进行,产生1-替代-4-三甲基-1,2,3-三醇.
- 该协议表现出高效率,为目标化合物提供高产量.
- 广泛的亚基质被成功使用,突出了该方法的多功能性.
- 反应成功地扩大到克数量,证明了它的实际应用性.
结论:
- 已开发出一种简单高效的点击反应方法,用于区域选择性合成4-trifluoromethyl-1,2,3-triazoles.
- 该方法在起始材料的可用性,稳定性和反应效率方面具有优势.
- 该协议为访问各种应用的三甲基化三醇衍生物提供了有价值的工具.
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