反-4-羟甲基哌啶-3-醇的合成  

Synthesis of trans-4-( Hydroxymethyl) piperidin-3-ol

作　　者：方教冰 陈雨辰 崔浩楠 王诗宇 刘明哲 Fang Jiaobing;Chen Yuchen;Cui Haonan;Wang Shiyu;Liu Mingzhe(School of Pharmaceutical Engineering,Shenyang Pharmaceutical University,Shenyang 110016)

机构地区：[1]沈阳药科大学制药工程学院

出　　处：《化学通报》2019年第7期663-665,共3页Chemistry

基　　金：国家自然科学基金项目(21875145);辽宁省自然科学基金项目(20180550392)资助

摘　　要：以4-羟甲基吡啶为原料,经苄基保护、硼氢化钠的还原、硼氢化氧化和脱苄基保护等四步反应得到新型5-羟色胺受体激动剂的关键中间体反-4-羟甲基哌啶-3-醇。总收率达55.7%。产物结构经IR、1H NMR和MS分析确证,并对合成工艺进行了优化。Trans-4-(hydroxymethyl)piperidin-3-ol,a key intermediate of novel 5-hydroxytryptamine receptor agonist candidate,was synthesized by 4-hydroxymethylpyridin as starting material through four reaction steps including benzyl group protection,reduction with sodium borohydride,hydroboration-oxidation,deprotection of benzyl group.The total yield was up to 55.7%.The reaction products were characterized by IR,1H NMR and MS,and the synthetic process was also optimized.

关 键 词：反-4-羟甲基哌啶-3-醇 硼氢化氧化 5-羟色胺受体激动剂 苄基保护 

分 类 号：TQ460.1[化学工程—制药化工]