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%.