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目的为加强对沙丁胺醇药物的质量控制,合成了欧洲药典中沙丁胺醇的两个杂质。方法分别以4-羟基苯乙酮和3甲-基-4羟-基苯乙酮为起始原料,经溴化、N-苄基叔丁基胺取代,再用H2/Pd-C脱去苄基,最后用硼氢化钠还原合成目标化合物。结果与结论目标化合物结构经1H-NMR、MS确证,合成的两种杂质可以作为沙丁胺醇药物质量控制的杂质对照品。该合成方法反应条件温和,原料易得,操作简单,收率高。
OBJECTIVE To improve the quality control of salbutamol, two impurities of albuterol in the European Pharmacopoeia were synthesized. Methods Starting from 4-hydroxyacetophenone and 3-methyl-4-hydroxyacetophenone respectively, bromination and N-benzyl tert-butylamine were used to replace them with H2 / Pd-C Benzyl, and finally reduction with sodium borohydride to synthesize the target compound. RESULTS AND CONCLUSIONS The structures of the target compounds were confirmed by 1H-NMR and MS. The two impurities synthesized could be used as impurity reference substance for albuterol quality control. The synthesis method has the advantages of mild reaction conditions, easy availability of raw materials, simple operation and high yield.