4-羟基-5,6,7,8-四氢-1,6-萘啶-2(1H)-酮的合成研究  

Synthesis of 4-hydroxy-5,6,7,8-tetrahydro-1,6-naphthyridin-2(1H)-one

作　　者：毛龙飞 许彩云 高原 毛伸 蒋涛 MAO Longfei;XU Caiyun;GAO Yuan;MAO Shen;JIANG Tao(School of Chemistry and Chemical Engineering,Henan Engineering Research Centerof Chiral Hydroxyl Pharmaceutical,Henan normal university,Xinxiang 453007,China)

机构地区：[1]河南师范大学化学化工学院河南省手性醇类药物工程技术研究中心化学制药及生物医用材料河南省工程实验室,河南新乡453007

出　　处：《化学研究与应用》2018年第6期985-988,共4页Chemical Research and Application

基　　金：新乡市科技攻关项目(CXGG16010)资助

摘　　要：本文以Boc-4-哌啶酮为原料,经过取代、还原、酰化、成环、脱保护等步骤得到医药关键中间体化合物4-羟基-5,6,7,8-四氢-1,6-萘啶-2(1H)-酮,总收率达到43%,并经过~1H NMR,^(13)C NMR和ESI-MS确定了所得化合物的结构。该合成方法具有操作简便,收率较高,纯度好,重复性好等优点,全过程无需经柱层析分离提纯,适合工业化大生产。With Boc-4-piperidone as a raw material,4-hydroxy-5,6,7,8-tetrahydro-1,6-naphthyridin-2（1H）-one was obtained via substitution,reduction,acylation,ring-formation,and deprotection in a total yield of 43%. The advantages of this method included a simple procedure,high product yield,and high purity. The method was very suitable for industrialmass production. The structures were characterized by proton nuclear magnetic resonance（^1H NMR）,carbon 13 nuclear magnetic resonance（^（13）C NMR）,and high resolution mass spectrometry（ HRMS）.

关 键 词：Boc-4-哌啶酮 4-羟基-5 6 7 8-四氢-1 6-萘啶-2(1H)-酮 工业化生产 

分 类 号：O626.4[理学—有机化学]