Synthesis of 1,7-dimethoxy-2-hydroxyxanthone,a natural product with potential activity on erectile dysfunction  

作　　者：Wen-Jing Liu De-Sheng Mei Wen-Hu Duan 

机构地区：[1]School of Pharmacy,East China University of Science and Technology [2]Department of Medicinal Chemistry,Shanghai Institute of Materia Medica.Chinese Academy of Sciences [3]Department of Medicinal Chemistry,Shanghai Institute of Materia Medica,Chinese Academy of Sciences

出　　处：《Chinese Chemical Letters》2013年第6期515-517,共3页中国化学快报（英文版）

基　　金：Financial support of the National Natural Science Foundation (Nos.81102461,81021062,and 90813034);National Science & Technology Major Project "Key New Drug Creation and Manufacturing Program"(Nos.2012ZX09301001-001 and 2012ZX09103101-024);the Shanghai Science and Technology Commission(Nos.11431921100 and 12DZ1930802)

摘　　要：The natural product,1,7-dimethoxy-2-hydroxyxanthone（1）,isolated from Securidaca inappendiculate Hassk,has a potential in the treatment of erectile dysfunction due to its significant relaxation activity on rabbit Corpus cavernosum.However,the isolation of compound 1 is problematic because of its high similarity in structure to its analogs.In this paper,the first synthesis of 1 was reported featuring two key reactions：a copper-catalyzed coupling reaction and an intramolecular cyclization.The natural product,1,7-dimethoxy-2-hydroxyxanthone（1）,isolated from Securidaca inappendiculate Hassk,has a potential in the treatment of erectile dysfunction due to its significant relaxation activity on rabbit Corpus cavernosum.However,the isolation of compound 1 is problematic because of its high similarity in structure to its analogs.In this paper,the first synthesis of 1 was reported featuring two key reactions：a copper-catalyzed coupling reaction and an intramolecular cyclization.

关 键 词：1 7-Dimethoxy-2-hydroxyxanthone Erectile dysfunction Synthesis Copper-catalyzed coupling reaction 

分 类 号：R284[医药卫生—中药学]