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目的合成抗痴呆药物4-乙酰氨基-N-(叔丁基)苯甲酰胺(CPI-1189)并优化其合成工艺。方法以4-硝基苯甲酸为起始原料,经过酰氯化、酰胺化、催化转移氢化和N-乙酰化4步反应合成目标化合物。结果目标化合物的总收率为67.9%,其化学结构经元素分析、1H-NMR、MS谱确证。结论与文献报道的方法相比较,本工艺以氯化亚砜为氯化剂,降低了成本,并改进了硝基还原反应工艺,缩短了反应时间,使操作条件更为简单、实用。
Objective To synthesize 4-acetylamino-N- (tert-butyl) benzamide (CPI-1189) as anti-dementia drug and optimize its synthetic process. Methods 4-Nitrobenzoic acid was used as the starting material to synthesize the target compound by acyl chloride, amidation, catalytic transfer hydrogenation and N-acetylation. Results The total yield of the target compound was 67.9%. Its chemical structure was confirmed by elemental analysis, 1H-NMR and MS spectra. Conclusion Compared with the methods reported in the literature, this process uses thionyl chloride as a chlorinating agent, which reduces the cost, improves the process of the nitro reduction reaction, shortens the reaction time and makes the operating conditions more simple and practical.