Synthesis of natural products or their analogs is interesting and challenging work. During the course of the investigation, chemists can not only prepare various kinds of bioactive compounds, but also discover new synthetic methodologies. The first chapter of this thesis deals with the development of modified methods to synthesize chrysosplenol B, chrysosplenol D, and their analogs. Both chrysosplenol B and chrysosplenol D have the flavone skeleton with 3-methoxyl and 5-hydroxyl groups. They have ability to potentiate the potent anti-malarial activity of artemisinin and have ability to potentiate the activity of norfloxacin. The second chapter deals with the synthetic effort towards 3-(carboxymethylthio)-picolinic acid and a functionalized analog. They were synthesized in order to determine the minimum structural requirements for activity. This may enable researchers to study the mechanisms of molecular recognition of phosphoenolpyruvate (PEP) and oxaloacetate (OAA) by cytosolic phosphoenolpyruvate carboxykinase (cPEPCK).