含氮杂环化合物的合成方法分析-有机化学专业论文.docxVIP

万方数据 万方数据 ABSTRACT Nitrogenous heterocyclic compounds play an important role in heterocyclic compounds, many chemists are enthusiastic about researching them due to their unique biological activity. 1,4-Dihydropyridines are a kind of important calcium channel blockers and widely used in the treatment of hypertension, angina pectoris, arrhythmia and other cardiovascular diseases. Nitrogenous four-membered ring compounds have special antibacterial activity and play an important role in many conversion reaction due to their special constrained structure. In addition, they also can be used as the intermediates to synthetize many amino acids, alkaloids and other natural or unnatural biological macromolecular compounds. Therefore, it is significant to study the novel synthetic methods of 1,4-Dihydropyridines and nitrogenous four-membered ring compounds. In this dissertation, our work is about developing novel synthethic methodologies, which can be specialized as the following: One-pot synthesis of 4-aryl-N-OH-Hantzsch esters A mild and convenient one-pot method for the synthesis of N-OH-Hantzsch esters was developed. The key step is controlling the first Michael addition at relatively lower temperature (0 oC) to prevent the further cyclization. To optimize the addition reactions for better yield, various solvents and bases were screened. Symmetrical and unsymmetrical N-OH-Hantzsch esters can be easily obtained in moderate yield using this methodology. Furthermore, the terminal hydroxyl group makes N-OH-Hantzsch esters be further transformed or introduced to other molecule easily for further investigation of the potential use in medicinal fields. The methodology is considered to be simple, gentle and with low cost. Study on the stereoselective synthesis of 1,3-diazabicyclo heptanes and heptenes in the presence of iodine We studied the one-pot preparation of 1,3-diazabicyclo heptanes and heptenes with high stereoselectivities from substituted amino diethyl malonates and cha