School of Pharmacy, Kitasato University, 5-9-1 Shirokane, Minato-ku, Tokyo 108-8641, Japan.
J Org Chem. 2011 Apr 1;76(7):2257-60. doi: 10.1021/jo1022487. Epub 2011 Mar 7.
Acetylcholinesterase inhibitor (-)-homogalanthamine 3 was synthesized from μ opioid antagonist naltrexone (2) in 16% total yield. The synthesis features Grob fragmentation as a key reaction, which was especially accelerated in the presence of 15-crown-5.
(-)-高丙氨酸 3 是从μ阿片受体拮抗剂纳曲酮(2)合成的,总收率为 16%。该合成的关键步骤是采用 Grob 断裂反应,在 15-冠-5 的存在下反应加速。