基拉尔-复合催化不对称 [3 + 2] 循环添加2'-基基与N-2,2,2-三甲基酸基胺的循环添加
Guo-Li Chai1, Xiao Wang1, Wei-Yu Huang1
1State Key Laboratory of Antiviral Drugs, Pingyuan Laboratory, School of Chemistry and Chemical Engineering, Henan Normal University, Xinxiang, Henan 453007, China.
The Journal of organic chemistry
|August 1, 2024
概括
一种新型不对称的循环添加反应有效合成复杂的螺旋氧醇衍生物. 这种方法提供了高产量和优秀的立体控制,用于创建具有四个立体中心的分子.
科学领域:
- 有机化学 有机化学
- 不对称的催化剂.
- 药用化学 医学化学
背景情况:
- 具有挑战性的合成复杂的性分子.
- 需要有效的方法来创建spirooxindole支架.
- 三甲基在药物发现中的重要性.
研究的目的:
- 开发一个高效的不对称 [3 + 2] 循环加法.
- 合成 3,2'-pyrrolidinyl spirooxindole 衍生物. 合成 3,2'-pyrrolidinyl spirooxindole 衍生物. 合成 3,2'-pyrrolidinyl spirooxindole 衍生物. 合成 3,2'-pyrrolidinyl spirooxindole 衍生物. 合成 3,2'-pyrrolidinyl spirooxindole 衍生物. 合成 3,2'-pyrrolidinyl 衍生物.
- 在反应中实现高立体选择性.
主要方法:
- 不对称的 [3 + 2] 循环加法反应.
- 使用的2'-基基和N-2,2,2-三甲基酸基胺.
- 使用一个 (R) -3,3'-I2-BINOL-复合物作为催化剂.
主要成果:
- 合成了广泛的螺旋氧醇衍生物.
- 实现了高产量 (高达>20:1 dr和>99% ee).
- 形成四个连续的立体中心,具有出色的控制.
结论:
- 开发了一个高效率和立体选择性的合成协议.
- 证明了温和的反应条件和广泛的基质范围.
- 能够获取有价值的三甲基替代的螺旋氧indoles.
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