C-S-选择性静态合使得立体定义的烯合成成为可能.
Jing Jing1, Ying Hu1, Zhenfeng Tian1
1Key Laboratory of Organic Synthesis of Jiangsu Province, MOE Key Laboratory of Geriatric Diseases and Immunology, Suzhou Key Laboratory of Pathogen Bioscience and Anti-infective Medicine, College of Chemistry, Chemical Engineering and Materials Science, Soochow University, 215123, Suzhou, China.
这项研究引入了催化静态交叉合反应,用于合成立体定义基. 该方法实现了高的CS选择性,使得药物发现应用的高效基构造成为可能.
科学领域:
- 有机化学 有机化学
- 催化剂是一种催化剂.
- 合成方法论 合成方法论
背景情况:
- 开发选择性交叉合反应对于复杂分子合成至关重要.
- 在Stille合器中控制位点和化学选择性仍然是一个挑战,特别是在不同的功能组中.
研究的目的:
- 开发一种高度选择性的C-S-Stille交叉合反应.
- 为了提供一个有效的路径,以立体定义的三和四替代基.
- 为了证明该方法在药物发现中的实用性.
主要方法:
- 帕拉催化Stille交叉合在酸酸盐和酸酸酸之间.
- 使用C-H硫化和C-S化进行选择性控制.
- 在交叉合中使用多 (伪) 烯.
主要成果:
- 在C-I,C-Br,C-Cl和C-OTf债券上实现了高的C-S选择性.
- 合成的立体定义的三和四替代基具有立体性.
- 证明了顺序和多重交叉合的选择性C-X功能.
结论:
- 开发的协议提供了对有价值的基基基因的方便访问.
- 该方法表现出广泛的功能组耐受性和选择性.
- 该协议适用于制药合成和药物发现中的烯基基因的模块化安装.
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