4-羟基-5,6,7,8-四氢-1,6-萘啶-2(1H)-酮的合成研究

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,13C 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(13C NMR),and high resolution mass spectrometry(HRMS).