Hydroxy-4 2(4fluoroaniline)5,6dimethyl pyrimidine.docVIP

 PAGE \* MERGEFORMAT 8 Hydroxy-4 2(4fluoroaniline)5,6dimethyl pyrimidine Of: Ding Bing, Ma Yuzhuo, WAY, Luo Yan, Liu Chang [Abstract] Objective To study potassium competitive acid blockers like hydrochloric Swiss cutting pull the synthesis of key intermediates. Methods of 4-fluoroaniline as starting materials under acidic conditions in the condensation with the amino nitrile formation N (4-fluorophenyl ) guanidine carbonate, the latter off the acid, then with methyl acetoacetate @ cyclization to give 4-hydroxy 2 (4-fluoroaniline) 5,6-dimethyl-pyrimidine. Results and conclusion The structure was confirmed by NMR NMR and MS characterization, the total yield was 73.6%, improved process is simple, suitable for industrial production. [Keywords:] K + competitive hydrochloric acid blockers like 4-hydroxy pull cutting Switzerland 2 (4-fluoroaniline) 5,6 Abstract: Objective To prepare 4 hydroxy 2 (4 fluoroanilino) 5,6 dimethylpyrimidine which is a key intermediate for the synthesis of an novel type of potassium competitive acid blocker, revaprazan hydrochloride. Methods The key intermediate was synthesized by using aminonitrile and 4 fluoroaniline as starting materials via guanidination, desalination as well as cyclization. Result and Conclusion The overall yield is 73.6%. The structure of the title compound was confirmed by 1H NMR and MS. The improved procedure is easy to scale up for its convenient operation. Keywords:: potassium competitive acid blocker, revaprazan hydrochloride; 4 hydroxy 2 (4 fluoroanilino) 5,6 dimethylpyrimidine, synthesis Swiss hydrochloride cutting Razan (revaprazan hydrochloride) is a South Korean company developed a new type of Yuhan potassium competitive acid blockers (potassium competitive acid blocker, P CAB), 2007 South Korea was awarded FDA clearance to market for the treatment of duodenal ulcers and gastritis. drug based on the potential inhibition of gastric acid secretion, with the traditional H + / K + ATP enzyme i