催化循环的o-Nitrothiophenols与Cyclohexanones到Phenothiazines的催化循环
Yinglin Zhao1, Jin Zhang1, Jingwu Zhang2
1Engineering Research Centre of Pharmaceutical Process Chemistry, Ministry of Education; School of Pharmacy, East China University of Science and Technology, 130 Meilong Road, Shanghai 200237, P. R. China.
The Journal of organic chemistry
|May 22, 2024
概括
一种新的催化方法直接将o-nitrothiophenols和cyclohexanones转化为. 这种高效的合成使用基组作为接受器和合剂,仅产生水作为副产品.
科学领域:
- 有机化学 有机化学
- 合成化学 合成化学
- 药用化学 医学化学
背景情况:
- 提亚是药物化学中至关重要的支架,特别是在抗精神病药物中.
- 现有的合成路线通常需要恶劣的条件,外部氧化剂或受体.
研究的目的:
- 开发一种新的,高效的,无氧化剂的方法来合成氨酸.
- 为了利用o-nitrothiophenols作为直接循环反应中的关键起始材料.
- 通过已知的药物的总合成来证明开发方法的合成实用性.
主要方法:
- 催化直接循环的o-nitrothiophenols与循环素的循环.
- 使用o-nitrothiophenols的基组作为内部受体和合剂.
- 作为反应的唯一副产品产生的水.
主要成果:
- 在没有外部氧化剂的情况下,从o-nitrothiophenols和cyclohexanones中成功合成表酶.
- 反应通过基的减少,C-H键的硫化和C-H键的脱水芳香化进行.
- 实现了抗精神病药物普罗马的三步总合成,展示了该方法的广泛合成价值.
结论:
- 新的催化循环化提供了一个高效和可持续的路径,以表.
- 该方法在内部使用基组的能力简化了反应并减少了浪费.
- 这种方法为合成多种类型的氨酸衍生物和相关化合物提供了显著的潜力.
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