五种苯乙醇胺类β受体激动剂的合成研究

Synthesis of Five kinds of Phenyl Ethanolamine β Agonists

以廉价的4-氨基苯乙酮为原料,通过苯环被溴化或氯化,再经腈化、α-氢溴化、有机胺胺化,最后通过硼氢化钾将羰基还原,可以得到溴布特罗、克伦特罗、西布特罗、西马特罗、溴氯布特罗5种苯乙醇胺类β受体激动剂。通过合成路线的合理设计,原料卤代反应后的中间体都可以作为后续反应的物料,原子利用率高,实现了绿色合成化学的目的。对产物结构经行了^11HNMR确认,其HPLC纯度在99%以上,可作为测定β受体激动剂的对照品试剂,满足食品安全的检测需求。

Five kinds of phenyl ethanolamine β agonists,including brombuterol,clenbuterol,cimbuterol,cimaterol,and bromoclenbuterol,were synthesized by using 4-aminoacetophenon as raw materials,which were obtained via benzene ring chlorination or bromination,cyanation,α-hydrogen bromination,amination with organic amines and reduction of carbonyl group by potassium borohydride.Through the rational design of the synthetic route,the intermediate of the halogenated reaction can be used as the material for the subsequent reaction,and the utilization of the atom is high,so as to achieve the purpose of green synthetic chemistry. The chemical structure of the products were confirmed by^1 HNMR,and their HPLC purity was above 99%.The obtained products could be used as reference reagents for determination of β agonists in food safety detection fields.