3,4-二取代基-β-苯乙胺盐酸盐类化合物的合成  

Synthesis of 3,4-Disubstituent Group-β-Phenethylamine Hydrochoride Compounds

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作  者:冯德日 韩翰[1] 刑辉[1] 冮岩[1] 范业明[1] 

机构地区:[1]沈阳医学院,沈阳110034

出  处:《科学技术与工程》2014年第21期1-4,共4页Science Technology and Engineering

基  金:沈阳医学院科技基金(20122035)资助

摘  要:3,4-二取代基-β-苯乙胺盐酸盐类化合物是四氢异喹啉类化合物合成过程中的一个重要中间体。以3,4-二羟基苯甲醛为原料,经溴代物取代,硝基甲烷缩合,NaBH4/BF3还原3步反应合成了该类目标化合物。考察了缩合反应及还原反应中各原料投料比、反应时间、反应温度对反应收率的影响。优化后平均反应总收率可达67.6%,且反应条件温和、避免了以往该类化合物合成过程中氰化钠等剧毒性物质的使用,产品经ESI-MS和1HNMR确证结构。3,4-disubstituent group-β-phenethylamines compounds is the very important intermediate of tetra- hydroisowuinolin compounds. 3,4-dihydroxyl group-benzaldehyde was substituted by bromoalkane, then the aldehyde was condensed with nitromethane, the product of the condensation was then reduced by sodium borobydride in the presence of boron trifluoride etherate to give the target compounds. The effects of agent proportion and reaction time ,reaction temperature on the yield of the condensation .reducing reaction were studied. After 3 steps, the average total yield could reach up to 67.6% , the reaction condition was mild, the reaction condition was mild, and sodium cyanide which was the violent in toxicity was avoided to use, the structure of the target compound was confirmed by means of ESI-MS and 1HNMR.

关 键 词:β-苯乙胺类化合物 四氢异喹啉 工艺研究 

分 类 号:O625.6[理学—有机化学]

 

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