The Synthesis And Anti-senil Dementia Effects Studies On The Derivates Of γ-Lactam 2-Substituted Esters

Clausenamide is isolated from aqueous extract of leaves of Clausena lansium. Base on the Pharmacological study, clausenamide could improve dysmnesia caused by multiagent including Aβ, enhance the efficacy of synapse, promote the formation of the new synapse, raise the activity of the cortex and the protein phosphatase of the Hippocampus and decrease the activity of mice serum ALT caused by CCl4. It can be used as nootropics or liver protectant. However, in water and most organic solvent, the dissolvability of clausenamide was low. Using clausenamide as the lead compound, four target compounds were designed in this article, for obtaining higher pharmacokinetics performance compounds.The synthesis of the lead compound and the derivates of the clausenamide was included in this thesis. Method of clausenamidone's separation was improved in the synthesis of the lead compound. In terms of ability, price acquisition and coproduct, corresponding organic acids were selected as acylating agents, DCC and DMAP were selected as catalysts. The better reaction routes were definited through studying the effect factor to the acylation reaction, for instance, the molar ratio of the reactant, reaction temperature, reaction time and postprocessing of the reaction, two intermediates and two target compounds were synthesized in the synthesis of the derivates. All of the target compounds were characterized by means of IR, 1H-NMR, MS and elemental analysis.