Chemosynthesis Of Hypericin

Hypericin is one of the most important active components of hypericum perforatum L. The study found that hypericin have significant effect of antidepression, inhibition central nerve, anticancer, antitumour, it also can inhibit antiretroviral replication. Hypericin is promising endogenous photosensitizer; it can be used knubbly diagnosis and therapy of photochemistry.As a little hypericin contain in Hypericum Perforatum L, the method of extraction and isolation is incomplete, so little hypericin has been got after extraction and isolation.At present, because the methods of extraction and chemosynthesis are imperfect, the content and yield of Hypericin is very low in the extracted and chemosynthesis product which is beyond of reqirment for exploitation of the terminal product. To solve the problems mentioned above, Hypericin was extracted and isolated from hypericum PerforatumL.And hypericin was synthesized by the chemosynthesis in the experiment. It has important meaning and clinical value of application that using the method of organic chemosynthesis synthesizes hypericin. So the study colligates literature date in and out of country. Chemosynthesis route was explored; some synthetically ethnics has been improved. Synthetically route has been designed as follows:1 The synthesis of 2-hydroxy-4-methyl benzoic acid This experiment adopts acetone and ethyl formate to synthesis formyl acetone. 2-hydroxy-4-methyl benzoic acid has been synthesized by formyl acetone and acetoacetic ester.2 The synthesis of 2-methoxy-4-methyl benzoic acid Using dimethyl sulfate as methyl reagent synthesize 2-methoxy-4-methyl benzoic acid.3 The synthesis of 2-methoxy-4-methylbenzoic chloride Methyl as protective group of hydroxy, the reagent sulfoxide chloride or phosphorus trichloride and 2-methoxy-4-methyl benzoic acid synthesize 2-methoxy-4-methyl benzoic chloride.