Synthesis Of Pimobendan's Derivatives

The serious damage of myocardial constringency dint may arouse chronic heart failure, the heart can not transport the blood to around place, and can not suffice the need of body metabolism. This kind of heart failure is called Congestive heart failure(CHF), which is a common disease. The cause of CHF is partly lacking blood of myocardial, high blood pressure, non-emphractic myocardial pathological changes, congenital heart attack and so on. Although in the mass the mortality of cardiovascular disease is decreasing, the mortality aroused by CHF is increasing continuously. So looking for a better drug for treating CHF is a cosmopolitan pop theme, and there are a lot of new drugs coming out.Pimobendan is a new inotropic agent with phosphodiesterase inhibiting and calcium-sensitizing effects. It came to the market in Japan in 1994. The present study indicated that it can descend the pressure of vas effectually, increase left ventricular ejection fraction.With analyzing the structure of pimobendan, the structure of benzimidazole and dihydropyridazinone is confirmed to be the essential active part. Owing to the worse water-solubility of this kind of drugs, theycan not be made into inject which affects the speed of effect. The author finds a better synthetic route of such compounds and designs ten unreported target compounds that consist of two levo forms which are synthesized with reasonably synthetic way and are identified by MS, IR, 1H-NMR and elemental analysis.