广谱驱虫药帕苯达唑的合成

The Synthesis of New Broad Spectrum Anthelmintic Parbendazole

关键词:  对正丁基苯胺  乙酰化  帕苯达唑  合成

Key words:  p,n-butylaniline  acylation  parbendazole  synthesis

摘要:

摘 要：以对正丁基苯胺为原料，经乙酰化、硝化、水解、还原、闭环反应合成了5-正丁基-2-苯并咪唑氨基甲酸甲酯（帕苯达唑）。首先将乙酰化和硝化合为一锅煮得到4-正丁基-2-硝基乙酰苯胺。再以甲醇作溶剂，碱性水解后直接以钯碳为催化剂，在40℃、0.5MPa条件下反应得到4-正丁基邻苯二胺。最后选用氰氨基甲酸甲酯为闭环剂制得目标产物。整个工艺流程简化了工艺条件，降低了生产成本，总收率可达41.8%，适合工业化生产。

Abstract:

Abstract: 5-butyl-2-benzimidazolecarbamic acid methyl ester ( parbendazole ) was synt- hesized from p,n-butylaniline. The process were acylation, nitration, hydrolysis, reductioncyclization. Fisrt acylation and nitration were held in one pot method to obtain 4-n-bu-tyl-2-niroacetanilide. Use methanol as solvent, after alkaline hydrolysis then use Pd/C as catalyzer at 40℃，0.5MPa to obtain 4-n-butyl-o-phenylenediamine. At last use methyl cyanocarbamate as cyclization reagent to obtain the final product. The process have lesstechnological conditions and lower costs. The overall yield was 41.8%. The process wassuitable for industrial production.