Study On The Synthesis Of 2-(4-fluorophenylsulfonyl)-ethylamine And Nicotinic Acid Derivatives

The amine-intermediates involved in the synthesis of the most pharmaceutical chemical products,as important chemical materials.In this paper,we studied the synthesis of three primary amines intermediates,2-(4-fluorophenylsulfonyl) ethylamine;2-aminonicotinic acid and 4-aminonicotinic acid,containing two parts as follows:Partâ… :Synthesis of 2 -(4-fluorophenylsulfonyl) ethylamine.This compound is a synthetic type of N-(Arylthioalkyl)-N'-(aminoalkyl)ureas and thioureas and oxidation derivatives,which are useful in the treatment of cardiac arrhythmia.It is prepared from ethanolamine by Gabriel Synthesis,via the Substitution, oxidation,hydrazine,and acidification,finally get 2-(4-fluorophenylsulfonyl) ethyl-amine hydrochloride,with a total yield of 21.4%.The process of this experiment is simple and easily separated without the use of column chromatogramphy,suitable for the enlarge produced.Partâ…¡:Synthesis of nicotinic acid derivatives.Nicotinic acid derivatives are important chemical intermediates.2-Aminonicotinic acid can be used for synthesis of a new generation of 5-hydroxytryp amine(5-HT) receptor agonism(SC-53606) and anti-bacterial,anti-inflammatory drugs,such as Nalidixic.4-aminonicotinic acid is mainly for ischemic cerebrovascular disease and sequelae,also used in the drug synthesis of thromboangiitis obliterans and phlebitis. In this paper,we obtained new synthetic routes as follows:the oxidation of quinoline and isoquinoline given the different pyridinedicarboxylic acid,dehydration by aceticanhydride,Hofmann reaction after ammonia to generate the target products,the total yield are 28%and 30%.