摘要
目的合成抗抑郁药西酞普兰中间体5-溴苯酞。方法以4-硝基邻苯二甲酰亚胺为原料,通过铁粉还原得4-氨基邻苯二甲酰亚胺,再经锌粉还原排氨得到5-氨基苯并呋喃-1-酮,最后经重氮化、溴代得5-溴苯酞,利用红外光谱确证结构。结果对各步反应条件进行考察,得出各步反应的最佳条件。结论本合成路线简便可行,原材料价廉易得,适合工业化生产。
OBJFLTIVE To synthesis 5-bromid benzofuran ketone,the key intermediate of citaopram. METHODS The target compound was prepared through reduction of 4-nitrophthalic imidine,discharging amine with zinc powder,diazotization and bromination. The products were characterized by FT-IR.RESULTS All the influent factors to each step have been discussed respectively, and the optimization condition have been obtained.CONCLUSION The synthesis route is convenient. Raw and processed materials are low-cost,and the process may be used in industry.
出处
《中国药学杂志》
CAS
CSCD
北大核心
2006年第24期1905-1908,共4页
Chinese Pharmaceutical Journal
关键词
还原
溴化
重氮化
5-溴苯酞
西酞普兰
reduction
bromination
diazotization
5-bromide benzofuran ketone
citalopram
