Study On The Synthesis Of 5-halonicotinic Acid And Its Derivatives

5-halonicotinic acid and its derivatives have special character and pharmaceutical activity, and they have a broad foreground of application. These compounds can inhibited cozymase synthesis from cozymase precursors and became a 'lethal synthesis'. These compounds used as anti-lipolytic agents, active in vitro reduced serum free fatty acids and lowered serum cholesterol. 5-halonicotinic acid and its derivatives effect on isoprenaline-induced myocardial necrosis and protected heart. These compounds can synthesize a novel chemical delivery system, and also as pharmaceutical compositions for treatment hyperproliferative disorders, such as: psoriasis, theumatoid arthritis, etc.The dissertation was included of three kind halo-substitute nicotinic acid derivatives. They were 5-chloronicotinic acid and its derivatives, 5-bromonicotinic acid and its derivatives, 5-fluoroicotinic acid and its derivatives, respectively.Synthesis of 5-bromonicotinic acid, 5-bromo-3-(2'-hydroxy-2'-propyl)-pyridine, 5-bromonicotinic acid ethylester, 3-actyl-5-bromo-pyridine, 5-bromo-3-(1'-hydroxy ethyl)-pyridine, respectively. These compounds were prepared using nicotinic acid as primal raw material, and improve upon the process of reaction to enhance the yield.5-aminonicotinic acid was prepared from 5-bromonicotinic acid and ammonium hydroxide solution through Amination Reaction in clave.Synthesis of 5-chloro nicotinic acid, 5-chloronocotinic acid ethyl ester, 5-chloronicotinamide, 5-chloro-3-cyanopyridine , 5-chloro-3-ethylamine-pyridine, 5-chloro-3-methanol-pyridine, respectively.5-chloronicotinic acid was obtained from 5-aminonicotinic acid in Sandmeyer Reaction.5-chloro-3-pyanopyridine was prepared using nicotinic acid as primal raw material, and this route of synthesis was not reported. The datum of 5-cholo-3- ethylamine-pyridine was not found.The synthetic method of 5-fluoronicotinic acid derivatives was similarly to 5-chloronicotinic acid derivatives. These compounds were 5-fluoronicotinic acid, 5-fluoronicotinic acid ethyl ester, 5-fluoronicotinamine, 5-fluoro-3-cyanopyridine,5-fluoro-3-formaldehyde-pyridine, respectively.5-fluoronicotinic acid was obtained form 5-aminonicotinic acid by Fluoration in Schiemann reaction. The condition of 5-fluoro-3-cyanopyridine had a critical betterment and result in a prodigious yield. About the datum of 5-fluoro-3-cyanopyridine was not found. The title compounds were identified by FTIR, GC/MS.