番荔枝宁合成工艺

以3,4-二甲氧基苯乙腈为起始原料,分别由水解和氢化还原制备3,4-二甲氧基苯乙酸和3,4-二甲氧基苯乙胺,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。该法合成番荔枝宁的总收率为47%。

Synthesis of Xylopinine

3,4-Dimethoxyphenylacetonitrile was employed as the starting material to prepare 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%.