番荔枝宁合成工艺研究

Ths Synthesis of Xylopinine

摘要:

以3,4-二甲氧基苯乙腈为起始原料，分别制备3,4-二甲氧基苯乙胺和3,4-二甲氧基苯乙酸，二者经酰化，Bischler-Napieralski环化，硼氢化钾还原制得中间体四氢罂粟碱，后同甲醛经Pictet-Spengler反应制得(±)-番荔枝宁。该方法合成番荔枝宁的总收率为47％。

Abstract:

3,4-Dimethoxyphenylacetonitrile was employed as the staring material to give 3,4-dimethoxyphenylethylamine and 3,4-dimethoxyphenylacetic acid via hydrolysis and hydrogenation reduction, respectively. The resulting two intermediates were reacted to produce the amide, which underwent Bischler-Napieralski cyclization, potassium borohydride reduction, and Pictet-Spengler reaction with formaldehyde to give racemic xylopinine in an overall yield of 47%.