Study On The Synthetic Technology Of Sivelestat Sodium Hydrate

Sivelestat sodium hydrate is a kind of drug which was exploited by Ono, it fits a kind of disease which named 'systemic inflammatory response syndrome ', for short 'SIRS'. The drug was approved on April 11,2002 in Japan and it was launched in June the same year. But in China, until a kind of epidemic disease called 'SARS' which was found in Guangdong province of China, and it's infectivity is so smart that can transmit pathogen through a short distance, lucubrating of the sivelestat sodium hydrate became. So the quantity of the drug can't meet market's want. That's the reason what the paper carry through the research.The preparation of sivelestat sodium hydrate of the paper is by glycin benzyl ester p-toluene sulfonic acid salt,p-hydroxybenzenesulfonic acid, pivoloyl chloride and o-nitrobenzoic acid as principle materials, Through a series of experiments, analysis, argumentation and comparing, the paper find out the difference of the three process, according the principle of convenient operation and cheapness and easy obtain so here select out the best one, the paper also discussed how to optimize the process.. After confirmed the process, the paper carrying through a series of experiments for studying reactive condition such as temperature, hour, rate of molar how to influence the rate of produce, so the paper find out the best condition that fits the experiment, and so the paper advanced the total yield from 35.24% on literature to 38.50%, some of operations become convenient also, at the same time the purity achieved the acquire of pharmacy, so the process fitter produce of industrialization.The paper summarized the research status of pharmacology, general pharmacology, toxicology and pharmacokinetics and clinical application of the drug, hinted the drug as a perfect pharmacy on the injury of lung and especially and probably of prophylactic and treatment on 'SARS' has a effective role so it has a capacious developing foreground.The product was authenticated by melting point, elemental analysis, IR spectrum, UV spectrum, MS spectrum, 1HNMR spectrum, 13CNMR spectrum, H-H cosy, C-H cosy, TGA-DSC, X-diffract, etc.