溴酪氨酸衍生生物碱沙海葵素A的简短高效全合成。

A short and efficient total synthesis of the bromotyrosine-derived alkaloid psammaplysene A.

作者信息

Xu Jingjing, Wang Kai, Wu Jinlong

机构信息

Laboratory of Asymmetric Catalysis, Department of Chemistry, Zhejiang University Hangzhou 310027 China

Department of Chemistry, Hangzhou Medical College Hangzhou 310053 China.

出版信息

RSC Adv. 2018 Apr 12;8(25):13747-13749. doi: 10.1039/c8ra02052c. eCollection 2018 Apr 11.

DOI:10.1039/c8ra02052c

PMID:35539328

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9079787/

Abstract

Psammaplysene A, an inhibitor of FOXO1a-mediated nuclear export, has been synthesized by a concise and improved route from tyrosine-derived acid and amine fragments which were easily constructed using commercially available -hydroxybenzaldehyde and tyramine as starting material, respectively. The strategy provides an efficient access of psammaplysene analogues that can be explored for potential pharmaceutical or biological activities.

摘要

沙马普林 A 是一种 FOXO1a 介导的核输出抑制剂，它已通过一种简洁且改进的路线从酪氨酸衍生的酸和胺片段合成，这些片段分别使用市售的对羟基苯甲醛和酪胺作为起始原料很容易构建。该策略为沙马普林类似物提供了一条有效的合成途径，这些类似物可用于探索潜在的药物或生物活性。