二氢呋喃和二氢吡喃2-位醚化的合成方法研究  

A Method for Etherification at 2-Position of Dihydrofuran and Dihydropyran

作　　者：杜芳瑜 杜洋 周启璠 陈国良[1] DU Fang-yu DU Yang ZHOU Qi-fan CHEN Guo-liang(Key Laboratory of Structure-Based Drug Design ＆ Discovery of Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, China)

机构地区：[1]沈阳药科大学基于靶点的药物设计与研究教育部重点实验室,辽宁沈阳110016

出　　处：《精细化工中间体》2017年第4期25-28,共4页Fine Chemical Intermediates

摘　　要：以对甲苯磺酸吡啶盐作催化剂,2,3-二氢呋喃和2,3-二氢吡喃为起始原料,与醇通过加成反应制备得到2-甲氧基四氢呋喃和2-(2-溴代)乙氧基四氢吡喃,并通过Gabriel伯胺合成法得到O-(四氢-2H-吡喃-基)羟胺。对甲苯磺酸吡啶盐催化的收率均在85%以上,其结构经1H NMR和MS确证。此法广泛应用于羟基和氨基的保护,具有操作简便、条件温和、原料成本低等优点。2-Methoxytetrahydrofuran and 2-（2-bromo）ethoxytetrahydropyran were obtained using 2,3-dihydrofuran or 2,3-dihydropyran as the starting material while p-toluenesulfonic acid pyridine salt as the catalyst. Meanwhile, O- （tetrahydro-2H-pyran-yl） hydroxylamine was prepared via Gabriel reaction. The structures were proved by 1H NMR and MS spectra, and the yield of target products were more than 85% .This method could be widely used in the protection of hydroxyl and amino groups with the advantages of simple operation, mild conditions, low cost of raw materials.

关 键 词：对甲苯磺酸吡啶盐 2 3-二氢呋喃 2 3-二氢吡喃 醚化 

分 类 号：TQ612.9[化学工程—精细化工]