Studies On The Synthesis Of Cs-Trihomocubane Ester/Amide Derivatives And Their Biological Evaluation

In the dissertation, the characteristics and the latest development of cubane, homocubane, Cs-trihomocubane and their derivatives are summarized. Their application in pharmaceutical synthesis was also mentioned. A series of Cs-trihomocubane amides/esters have been synthesized and their biological activity has been evaluated.On the basis of reports on Cs-trihomocubane compounds, the best scheme to prepare Cs-trihomocubane-8-ol and Cs-trihomocubane-8梐mide are chosen. Then five of their amides and five esters have been synthesized. They are Benzoic-Cs-trihomocubane-8-ester(TMl); 4-nitro-benzoic-Cs-trihomocubane-8-ester (TM2);4-bromide-benzoic-Cs-trihomocubane-8-ester(TM3);l-acetyloxy-3-trifluorom ethyl-benzoic-Cs-trihomocubane-8-ester(TM4);3-pyridine-monocarboxylic-Cs-triho mocubane-8-ester(TM5);4-bromo-benzoic-Cs-trihomocubane-8-amide(TM6);2,4,6-tri methoxy-benzoic-Cs-Trihomocubane-8-amide(TM7);3-pyridine-monocarboxylic-Cs-trihomocubane-8-amide(TM8);4-nitro-benzoic-Cs-Trihomocubane-8-am ide(TM9); Benzoic-Cs-trih-omocubane-8-amide (TM10).This work is the beginning of studies on Cs-Trihomocubane derivatives as biomedical agents. It has created opportunities for pharmaceutical development in the future.