CAJ | 학술논문

目的：改进醋酸巴多昔芬的合成工艺。方法：以对羟基苄醇和环己亚胺基乙基氯盐酸盐为起始原料，经过亲核取代、氯代得到侧链，4-苄氧基苯丙酮和4-苄氧基苯肼盐酸盐经缩合得母核，侧链和母核缩合后，经成盐，氢解、中和，与乙酸成盐总计6步得目标化合物。结果：目标化合物经质谱、核磁共振确证其结构。总收率可达53％，产品高效液相色谱法（HPLC）获得纯度可达99．5％以上。结论：改进后的工艺步骤大大缩短，且操作简单，醋酸巴多昔芬收率和纯度较高，适合工业化生产。
목적：개진작산파다석분적합성공예。방법：이대간기변순화배기아알기을기록염산염위기시원료，경과친핵취대、록대득도측련，4-변양기분병동화4-변양기분정염산염경축합득모핵，측련화모핵축합후，경성염，경해、중화，여을산성염총계6보득목표화합물。결과：목표화합물경질보、핵자공진학증기결구。총수솔가체53％，산품고효액상색보법（HPLC）획득순도가체99．5％이상。결론：개진후적공예보취대대축단，차조작간단，작산파다석분수솔화순도교고，괄합공업화생산。
Objective: To improve the synthetic process of bazedoxifene acetate.Methods:The side chain was synthesized from 4-hydroxybenzyl alcohol and 2-( hexamethyleneimino) ethyl chloride hydrochloride as starting materials through nucleophilic substit-uent and chlorination.The stemnucleus was obtained by condensation taking 4-benzyloxypropiophenone and 4-methoxyphenyl-hydrazine hydrochloride as raw materials; the side chain and the stemnucleus were condensed and process by acidification,hydro-genolysis,neutralization and acidification with acetic acid to get the target compound via total six steps.Results: The structure of the target compound was confirmed by ESI-MS and 1H-NMR.The total yield was 53%,and the High Performance Liquid Chromatogra-phy (HPLC) purity was more than 99.5%.Conclusion:The improved process of bazedoxifene acetate with short steps, simple op-eration,good yield and purity is feasible for industralization.