The Synthesis Process Research Of Aminine As Antihypertensive Drug

Hypertension is the most common cardiovascular diseases among older people. Due to the influence of various factors, the age of hypertensive patients are greatly reducted, even many young people are suffering from high blood pressure.High blood pressure serious damage the human’s health. Laminine is a basic amino acid that was discovered from kelp, which has pharmaceutical function of lowering blood pressure and blood lipid, and which can prevent hypertension and cerebral hemorrhage. Laminine, which has not been listed at home and abroad at present, is a new category drug of China. Laminine is rarely contented in the kelp. If Laminine is extracted from kelp, it will cause a lot of pollution. The cost of this method is too high so it has no industrial production value. The chemical synthesis method was used to prepare an antihypertensive drug-laminine. Aiming to achieve the clean production, a safe and low toxic green chemistry-DMC was used as raw material, and the response surface methodology was used to analyzed various factors influencing the reaction to optimize the preparation technology.The method of metal chelate was adopted to protect a-amino of lysine selectively. Lysine metal chelate was synthesized respectively by five kinds of metal ion-calcium, magnesium, copper, zinc and nickel and lysine as raw materials. By studying these reactions copper ions was used as a-amino protective agen. Through the single factor experiment, the best three factors which can effect the reaction on yields are found to be the reaction temperature, time and pH of system, and the process was optimized by response surface methodology. The best condition of preparation process is:the reaction temperature of 66℃, time of 2 hours, pH=7.5. Lysine copper can be separated and purified by 80% ethanol aqueous solution. The maximum yield is 93.15%.Secondly, In the preparation experiments of ε-N trimethyl lysine the DMC was used as methylating reagent.This paper also explored the influence of temperature, time, catalyst, reaction system and phase transfer catalysts on the methylation reaction. With the single factor experiment and the response surface methodology,the preparation technology of ε-N trimethyl lysine was optimized. The best condition of preparation process is:the reaction temperature of 111℃ , acetone dosage of 29%, time of 3.5h. The maximum yield is 54.70%, which is 9% higher than before.Finally, the paper comprehensively used distillation, extraction and column chromatography methods to isolate and purify the mixed solution. The optimum reaction conditions are discussed through the static adsorption test: optimal adsorption pH=5.0, adsorption time of 30min, adsorption temperature of 25％ and the initial elution pH=10.0. Then the methylation products were purificed by 732 cation exchange resin on this basis. The best eluent is dilute aqua ammonia, pH=10.8. And the TLC, melting point determination and IR technique were used to identify the laminine.