The most important two features of a successful drug are the biochemical effects of active pharmaceutical ingredients and the efficacy of their delivery methods. Synthetic organic chemistry plays crucial roles in virtually both of these aspects for the design and the development of new drugs. Herein, in the first half part of the dissertation, a novel synthesis strategy of sulfamate esters is developed, which has been successfully applied into the synthesis of several tripartate pro-drugs with

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... he purpose of improving the delivery efficiency of ethinyl estradiol. Their pharmaceutical effects are evaluated by both in vitro and in vivo studies as described. In the second half part, novel synthesis of several biomimetic enzyme inhibitors, including selenoxide, diselenide, seleninic acid, and various other organoselenium compounds is reported. Evaluation of these biomimetics will be elucidated in the future.