广东药科大学学报2025，Vol.41Issue(5)：37-41,5.DOI:10.16809/j.cnki.2096-3653.2025071501
盐酸溴己新的合成工艺研究
Optimization of the synthetic process for bromhexidine hydrochloride
王栋 1张月红 1罗鹏 1赵亮 1李友军 1胡刚 1胡凯1
作者信息
- 1. 江苏润安制药有限公司,江苏 淮安 223299
- 折叠
摘要
Abstract
Objective To optimize the condensation reaction process in the synthetic route of bromohexidine hydrochloride.Methods Using 2-amino-3,5-dibromobenzoic acid(SM1)as the starting material,the intermediate state 2-amino-3,5-dibromobenzoyl anhydride(XJ-1)was synthesized via the anhydride method by reacting SM1 with trimethylacetyl chloride.XJ-1 subsequently underwent nucleophilic addition with N-methylcyclohexylamine(SM2)to yield the bromhexine hydrochloride intermediate(XJ-2).XJ-2 was then subjected to amide reduction followed by salt formation to obtain the final product,bromhexine hydrochloride.Results The target compound was confirmed by 1H-NMR/13C-NMR/MS,and elemental analysis.The condensation reaction achieved a yield of 65.41%.Conclusion The novel process eliminates the need for stringently regulated chlorination processes,avoids toxic gas emissions,and reduces both safety risks and environmental remediation costs.Featuring mild reaction conditions,cost-effective implementation(without expensive coupling reagents),and excellent reaction selectivity,this approach demonstrates strong potential for industrial-scale production.关键词
盐酸溴己新/祛痰止咳/酸酐法/合成Key words
bromhexine hydrochloride/dispelling phlegm and relieving cough/anhydride method/synthesis分类
医药卫生引用本文复制引用
王栋,张月红,罗鹏,赵亮,李友军,胡刚,胡凯..盐酸溴己新的合成工艺研究[J].广东药科大学学报,2025,41(5):37-41,5.
