Department of Medicinal Chemistry, School of Pharmacy, The University of Kansas , Lawrence, Kansas 66045, United States.
Org Lett. 2017 Oct 6;19(19):5414-5417. doi: 10.1021/acs.orglett.7b02684. Epub 2017 Sep 14.
Informed by previous semisynthetic work on salvinorin A, a modular total synthesis has been developed capable of producing novel compounds targeting the κ-opioid receptor. The strategy has permitted the deliberate simplification and introduction of functionality about the target molecule to provide access to molecular features on salvinorin A otherwise unattainable by semisynthesis. Using this approach, a potent pseudo-neoclerodane κ-opioid receptor ligand (2) has been realized.
受以前对 salvinorin A 的半合成工作的启发，开发了一种模块化的全合成方法，能够产生针对 κ-阿片受体的新型化合物。该策略允许对目标分子进行故意简化和功能化，从而获得 otherwise unattainable 通过半合成获得的 salvinorin A 的分子特征。使用这种方法，实现了一种有效的假新茄碱 κ-阿片受体配体 (2)。
