Facile synthesis of acacetin and its derivatives

Yuan Zhao; Li Cai; Qiang Sui; Feng Lin; Wen Jiang; Jianli Chen; Weigeng Lu; Qi Gao

doi:10.1016/j.bmcl.2016.06.018

Facile synthesis of acacetin and its derivatives

Bioorg Med Chem Lett. 2016 Aug 1;26(15):3577-80. doi: 10.1016/j.bmcl.2016.06.018. Epub 2016 Jun 9.

Authors

Yuan Zhao¹, Li Cai², Qiang Sui¹, Feng Lin¹, Wen Jiang³, Jianli Chen¹, Weigeng Lu⁴, Qi Gao⁵

Affiliations

¹ China State Institute of Pharmaceutical Industry, 285 Gebaini Road, Shanghai 200120, China.
² Division of Mathematics and Science, University of South Carolina Salkehatchie, Walterboro, SC 29488, United States. Electronic address: CAILI@mailbox.sc.edu.
³ China National Pharmaceutical Industry Information Center, 1320 West Beijing Road, Shanghai 200040, China.
⁴ China State Institute of Pharmaceutical Industry, 285 Gebaini Road, Shanghai 200120, China. Electronic address: sipiluwg@163.com.
⁵ China State Institute of Pharmaceutical Industry, 285 Gebaini Road, Shanghai 200120, China. Electronic address: gao.qi@sipi.com.cn.

PMID: 27321812
DOI: 10.1016/j.bmcl.2016.06.018

Abstract

Acacetin, a O-methylated bioflavonoid isolated from the traditional Chinese medicine Xuelianhua (Saussurea tridactyla), is a promising orally effective atrium-selective antiarrhythmic agent for the treatment of atrial fibrillation (AF). Here we describe an efficient two-component method for the synthesis of acacetin and its derivatives.

Keywords: Acacetin; Atrial fibrillation; Catalysis; Flavones; Fries rearrangement; Synthesis.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Flavones / chemical synthesis*
Flavones / chemistry
Medicine, Chinese Traditional
Molecular Structure
Saussurea / chemistry*

Substances

Flavones
acacetin