Synthesize And Study On Rocuronium Bromide

Rocuronium Bromide was empoldered successfully by Organon and came into market in 1994 as an aminosteroid non-depolarizing muscle relaxant. It is one of the most commonly prescribed muscle relaxants in the USA, Canada and the majority of European countries.Rocuronium Bromide has an intermediate duration of action. Its rapid onset of action: around one minute compared to two to three minutes for most other modern muscle relaxants. This helps minimize risks to the patient. Also it has rapid recovery characteristics:Patients recover more rapidly even after long and complicated operations. And it has shown little or no effect on heart rate or blood pressure and virtually no histamine release.Rocuronium Bromide is a promising muscle relaxant and it gets the attention of pharmacy aboard. At present,there is no report about the synthetical technics of rocuronium bromide. In this paper,the first four parts in the six parts technics have been completed. The main reserch work is shown below:1,Through a large number of literature survey,two main of the route were found out and one of the route which was fit for the industrial production was the best one. Fourthermore,the influencing factors of each reaction was investigated deeply. The original material was cheepness and made in Chinese domestic market .2,In the process of synthesizing the original material 2α,3α,16α,17α-epoxy-5α-androstane- 17β-acetyl,the best reaction conditions were explored after repeated research and testing on the basis of the original patent. The yield raised from 25.2 to 40.7%,much higher than the original patent.3,The route was deeply and carefully discussed. The main reaction factors,such as activator,reaction time,temperature are entirely discussed and compared. So the most desired industrial conditions are selected.4,(2β,3α,5α,16β,17β)-2-(4-morpholinyl)-16-(1-pyrrolidinyl)-androstane-3,17-diol was obatained by 5α-androst-2-ene-17-one,as the original material, reacting with isopropenyl acetate; then oxidized by 3-cloroperoxybenzoic acid,after that refluxed in pyrrolidine some minutes; deoxidised by sodium brohydride;then refluxed in morpholine for three days. The resulting product was characterized by MS,elementary analysis,melting point,degree than polarimet.