2-(邻羟基苯基)吡咯烷的合成

2-(邻羟基苯基)吡咯烷的合成
摘要：2-(邻羟基苯基)吡咯烷作为一类重要的药物中间体和潜在的有机催化剂，本文介绍了一类适合放大制备它的方法。以水杨酸为原料，通过酸的酯化反应，酚羟基的甲基保护，缩合，水解，碱化制备到亚胺底物，然后还原，脱甲基保护基，合成出目标产物，具体合成路线如下。

关键词：2-芳基吡咯烷，合成
 
Synthesis of 2-(pyrrolidin-2-yl)phenol
 

Abstract: As a kind of important drug intermediates and the potential organocatalysts, herein we  introduced a method on the synthesis of 2-(pyrrolidin-2-yl)phenol and this method was very suitable for large scale preparation of 2-(pyrrolidin-2-yl)phenol. The starting material was 2-hydroxybenzoic acid . After the esteration to acid and Methyl protection to phenol, it was transferred to compound 2. It reacted with NVP, and then compound 3 was obtained. After hydrolysis in the con. HCl solution of compound 3 , the solution was adjusted to PH 12 to yield the imine 4. The imine 4 was reduced with NaBH4, and then deprotection of Methyl to yield the target product. Synthetic route was showed below.

Key word: synthesis, 2-(pyrrolidin-2-yl)phenol, drug intermediates

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