Synthesis Of Agomelating Related Substances And Content Determination Of Tauroliding Solution

Agomelating is a kind of naphthalene derivatives of melatonin,the chemical name is N-[2-(7-methoxy-1-naphthyl)ethyl] acetamide.It offers better treatment results to all types of depression and has fewer side effects.Controlling the purity of drugs is an important prerequisite to ensure the safety and effectiveness of drugs.Ensuring the content of impurities is important factors to control drug purity but also to control drug safety and effection.At present,we have synthesized four related substances of agomelatine.They were 2-(7-methoxy-1-naphthyl)ethylamine,2,2,-bis(7-methoxy-1-naphthyl)diethylamine,NN-bis(2-(7-methoxy-1-naphthyl)ethyl)acetamide,N-(2-(7-methoxy 3,4-dihydro-1-naphthyl)acetamide.In which the 2-(7-methoxy-1-naphthyl)ethylamine uses 7-methoxy 3,4-dihydro-1-naphthalenone as raw material,it is produced by the addition of cyanide with acetic acid,DDQ dehydrogenation,and Li Al H4 reduction reaction.2,2,-bis(7-methoxy-1-naphthyl)diethylamine uses 7-methoxy 3,4-dihydro-1-naphthalenone as raw material,it is produced by the addition of cyanide with acetic acid,DDQ dehydrogenation,and hydrogenation reaction of Raney nickel.N N-bis(2-(7-methoxy-1-naphthyl)ethyl)acetamide is produced by adamidation reaction on the basia of the synthesis of 2,2,-bis(7-methoxy-1-naphthyl)diethylamine.N-(2-(7-methoxy 3,4-dihydro-1-naphthyl)acetamide uses 7-methoxy 3,4-dihydro-1-naphthalenone as raw material,it is produced by the addition of cyanide with acetic acid,reduced by Li Al H4,and amidation reaction.Tauroliding is a broad-spectrum antibiotic,it can be used for clinical treatment of infectious diseases.Tauroliding has good bactericidal and antiendotoxin effect,because of the nature of hydrolysis in aqueous solution of formaldehyde,taurultam.Therefore,we adopt two methods to determine the content of Tauroliding solution.Spectrophotometer and HPLC,the method of spectrophotometer was used to chromotropic acid to capture formaldehyde,the derivatives(with conjugatedstructure),derivatives can be detected,and then the content was determined.HPLC used pre column derivatization,Naphthalene sulfonyl chloride derivatives taurultam fragment which was decomposed in tauroliding aqueous solution.Producting formation can be detected,then determine the content.