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Synthesis Of Nicotinic Acid Derivatives

Posted on:2006-12-01Degree:MasterType:Thesis
Country:ChinaCandidate:Z X LiuFull Text:PDF
GTID:2121360155458736Subject:Applied Chemistry
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Nicotinic acid derivatives are a series of intermediates of fine industry and Pharmaceuticals. They are material for manufacture of medicines, agrochemicals, dyes and so on. Synthesis of nicotinic acid derivatives is significant to develop and reform the structures of new medicines.The synthesis of nicotinic acid derivatives is improved in the article. ① Nicotinamide-N-oxide (Ⅰ) was prepared by oxidizing nicotinamide in AcOH by 30% H2O2. The reaction conditions recommended are the molar ratio of Nicotinamide to H2O2 is 1:1.5, amount of AcOH is 50ml (amount of nicotinamide is 5.0g), reaction time is 4h and the yield is 80.6%; And treatment of ( Ⅰ ) with a mixture of phosphorus pentachloride and phosphorus oxychloride gave 2-chloronicotinonitrile. The reaction conditions recommended are the molar ratio of Nicotinamide-N-oxide to phosphorus pentachloride , phosphorus oxychloride is l:1.7:5.0,reaction time is 2.0h and the yield is 48.9%.② nicotinic acid 4-acetylamino-phenylester was synthesized from nicotinic acid with paracetamol by the ester bond; ③ nicotinic acid N-oxide was prepared by Oxidizing nicotinic acid in AcOH by 30% H2O2; ④ 5-substituted nicotinic acids were prepared using nicotinic acid as starting material; ⑤ synthesis of 5-fluoronicotinic acid via nitration and fluorodenitration of nicotinic acid also has been investigated.
Keywords/Search Tags:nicotinic acid derivatives, 2-chloronicotinonitrile, 4-acetylamino-phenyl nicotinate, 5-fluoronicotinic acid, nicotinic acid N-oxide, synthesis
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