Based on methylthio acetamide for synthesis of Nepafenac
Abstract: Non-steroidal anti-inflammatory drugs (NSAIDS) anti-inflammatory, allergy and pain, and no steroids adverse reactions, therefore, its application in the eye of the growing importance. But several non-steroidal anti-inflammatory drug in use process with certain side-effects. In order to reduce adverse reaction, and seek safety and effective anti-inflammatory drugs, in recent years, domestic and foreign scholars of non-steroidal anti-inflammatory drug eye application research, think of its structure reform or precursor drug is the effective way to reduce adverse reactions.
Nepafenac is a new generation of nonsteroidal anti-inflammatory drugs used to treat cataract surgery, mainly between pain and inflammation. In the eye, drug can quickly through the cornea, and in the eyes of the hydrolysis enzyme organization under into fenway ammonia acid, it can quickly reach sites. This paper main job is to Nepafenac synthesis by methylthio acetamide, and on this basis, the scale expansion in the problems in the course of difficulty. After many experimental study，we found that in hypochlorite tert-butyl diazoacetate synthetic process，the most prolific rate is: to avoid light environment, use liquid temperature control to zero, the reaction time for 5 minutes; In the process of synthesis of ethyl amide linked armor, ethyl amide chlorine add 20 minutes can effectively prevent the critical boiling; In the process of synthesis of Nepafenac，defecate tert-butyl diazoacetate dropping time has the most prolific rate for 30min.
Keywords: Nepafenac; Non-steroidal anti-inflammatory drug; Methylthio acetamide
