Studies On The Synthesis Of D₃-Trihomocubane And Homocubane Amide And Ester Derivatives And Biological Evaluation

In this dissertation, we summarized the characteristics amd the latest development of cubane, homocubane, D3-trihomocubanc and their derivatives. Their application in pharmaceutical synthesis was also mentioned. A series of D3-trihomocubane and homcxubane amides and esters have been synthesized and their biological activity has been evaluated.On the basis of reports on D3-trihomocubane and homocubane compounds, we chose the best route to prepare D3-trihomocubane-7,1 I梔iol and D3-trihoniocubane-7,1 1梔iamine and homocu-bane -2,4 -diacid.Then five of their amides and five esters have been syr~hesized. They are 4-bromo-benzoic acid D3-Trihomocubane-7,1 1-diester (TM1); 4-iodo-benzoic acid D3-Trihomocubane-7,1 1梔iester (TM2); 4-nitro-benzoic acid D3-Trihomocubane-7, 11 -diest~r (TM3); 3,5-Bistrifluoromethyl-b-enzene acetic acid D3-Trihomxubane-7,I 1-diester (TM4); 7,11- (4-bromo-benzamido) -D3-Triho-mocubane (TM5); 7,1 1-(4-iodo-benzamido)-D3-Trihomocubwie (TM6); 7,11- (4-nitro--benzamid-o) -D3-Trihomocubane(TM7); N-(3,5-Bistrifluoromethyl)phenylhomocubane-2,4-diamide(TM8); N-Tetrahydro- I ,4-oxazinylhomocubane-2,4-diamide (TM9); homocubane-2,4-(phenyl) diester (TM1 0). IR and 11-I-NMR have confirmed their structure.We have submitted these compounds for preliminary biological-activity screening.The result showed that TM8 can inhibit cancer of the lung and the colon.The work is the beginning of studies on D3-Trihomocubane and homocubane derivatives as biomedical agentsit has created opportunities for pharmaceuti~I development in the future.