摘要
为提高常用抗癫痫药丙戊酸钠的质量,合成了它的有关物质2-异丙基戊酸(1)。用氰乙酸甲酯(2)和溴丙烷在甲醇钠的甲醇溶液进行烷基化反应得到2-氰基戊酸甲酯(3)。3和2-碘丙烷在甲醇钠的甲醇溶液中反应得到2-氰基-2-异丙基戊酸甲酯(5)。5经硫酸水解、脱羧,再经氢氧化钠水解和硫酸酸化得到1,总收率约4%,纯度98%。
To improve the quality of sodium valproate,a commonly used anti-epileptic drug,its related substance 2-isopropyl pentanoic acid(1)was synthesized.The compound methyl 2-cyano-valerate(3)was obtained by the reaction of methyl cyanoacetate(2)and bromopropane in methanol solution of sodium methoxide.And then,3 was reacted with 2-iodopropane in methanol solution of sodium methoxide to synthesize methyl 2-cyano-2-isopropyl valenate(5).Followed by hydrolysis and decarboxylation,hydrolysis with sodium hydroxide and acidification with sulfuric acid,the title compound 1 was obtained with a total yield of 4%and the purity of 98%.
作者
魏正华
WEI Zhenghua(Shanghai Qingping Pharmaceutical Co.,Ltd.,Shanghai 201799)
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2023年第5期739-741,共3页
Chinese Journal of Pharmaceuticals
关键词
丙戊酸钠
杂质
2-异丙基戊酸
合成工艺
sodium valproate
impurity
2-isopropyl pentanoic acid
synthetic process