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。 |
关键词: 对正丁基苯胺 乙酰化 帕苯达唑 合成 |
DOI: |
投稿时间:2008-03-18修订日期:2008-04-17 |
基金项目: |
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The Synthesis of New Broad Spectrum Anthelmintic Parbendazole |
furui |
(Institute of Fine Chemical Engineering) |
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. |
Key words: p,n-butylaniline acylation parbendazole synthesis |