Study On Synthesis Of Intermediate Of Marine Alkaloid Baculiferin L As Anti-HIV-1 Activity

AIDS is a kind of systemic immune dysfunction syndrome caused by the human immunodeficiency virus infections.Since 1981,the first case of AIDS was found,more than 30 million people has died of AIDS which was called "Plague of the century".AIDS has become one of "the four killers" threatening the public health.The increasing number of infection by HIV has become a serious threat to the public health of the world.Therefore,the research and development of Anti-HIV drugs has been paid more and more attention by pharmacologists.Baculiferin L is a kind of alkaloids that extracted from the South China Sea Sponge Iotrochota baculifera.This compound has novel structure and shows significantly physiological activity target on HIV-1.The preliminary study of mechanism showed that Vif?gp41 and APOBEC 3G may be the targets of Baculiferin.Up to now,there is no anti-HIV drugs on sale aims at these three targets.Obviously,the synthesis of Baculiferin L has vital practical significance.This paper mainly studies on the synthetic process of the baculiferin L intermediate,and the establishment of their Content analysis method.Our synthetic process begins with the 3,4-dimethoxy benzaldehyde that is cheap and easy to get,undergoes Darzens condensation,alkaline hydrolysis,decarboxylation,pyrrole synthesis,Fu-gram respectively,hydrolysis,Cyclization reaction to get all the intermediates with the detection of the reaction process by HPLC analysis method and trials of recrystallization in order to get these intermediate easily.These works will provide experimental basis for the large-scale preparation and industrialization production of baculiferin L,a lead compound with Anti-HIV-1 activity from the ocean in the future.