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.
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)