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Stereoselective Synthesis of Cyclopropane Carboxylic Acid

有机合成与工艺文献分享 2025-05-19 08:04
文章摘要
本文主要研究了环丙烷羧酸的立体选择性合成方法。背景方面，研究指出使用含缩醛手性辅基的底物时，由于产率低和立体选择性差而未能成功。研究目的是通过双Heck偶联反应合成目标产物，并探讨钯催化过程中可能出现的消旋化问题。研究结论表明，采用银碱的阳离子机制可提高反应活性和选择性，通过计算分析确定了有利的二氯环丙烷化选择性，最终优化工艺实现了目标产物1的高效合成，总收率达13%，纯度97.8%，对映体过量值>99.5%。
Stereoselective Synthesis of Cyclopropane Carboxylic Acid
查看文献： Design, Development, and Scale-Up of a Stereoselective Synthesis of (1R,3R)-3-(3,5-Bis(trifluoromethyl)phenyl)-2,2-dichlorocyclopropane Carboxylic Acid
查看期刊：Organic Process Research & Development
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