The Synthesis And Studies Of Series Aromatic Nucleus Derivational Medicine Intermediate Ⅱ

As an important part of fine chemical field, medicine industry have became the focal point of many countries' development and competition. With the progress of the science and technology, more and more new medicines have been developed to benefit human beings. As the improving of people's living standard, the requirement of new medicine is increasing rapidly. New exploitation of medicines depended on the high quality of new medicine intermediate' development, therefore their research is of great significance.In this thesis, in order to find some novel medicines, we designe and synthesize nine important aromatic nucleus derivational medicine intermediates. The thesis includes five chapters as follows:In chapter one we address some development status of medicine intermediates, and through review some current hot spots, the main targets and contents of this research were put forward.In chapter two we synthesized 5-Amino-3-(4-pyridyl)isoxazole, which is the intermediate of malonyl coenzyme A decarboxylase inhibitors for ischaemic heart disease treatment, and determine it by single-crystal X-ray diffraction.In chapter three, in order to get two cyclic nucleotide phosphodiesterases inhibitors that is PDE3B and PDE5 inhibitors therapy for heart failure and male sexual dysfunction, we prepared their intermediate: 4-Bromo-2-methylbenzaldehyde and 4-Methoxypiperidine hydrochloride respectively. Besides the conventional testing, 4-Methoxypiperidine hydrochloride was tested by single-crystal X-ray diffraction.In chapter four we synthesized three arylboronic acids as the intermediates of the chiral biaryl compounds: that is 3-Chloro-4-pyridylboronic acid, Qinoline-4-boronic acid and Qinoline-6-boronic which are the chiral biaryl compounds' intermediates.In chapter five we synthesized three pyridyl-hydrazines that is 3-Hydrazinopyridine hydrochloride, 2-Chloro-3-hydrazinopyridine hydrochloride and 6-Methyl-2-hydrazinopyridine hydrochloride. respectively. Through modify technology for preparation those compounds, not only the yields are higher, but also reduce the cost and pollution of environment significantly.