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目的设计合成新型抗过敏药物依巴斯汀的人体活性代谢产物——羟基依巴斯汀。方法以苯甲酰氯为原料,经付克酰基化、还原和置换反应得到中间体二苯基溴甲烷(4);再以α,α-二甲基苯乙酸为原料,经过5步反应得到中间体9;中间体4和中间体9经缩合、水解反应得到目标产物。结果与结论目标化合物的总收率为21.0%,其结构经1H-NMR谱和M S谱确证,纯度经HPLC测定达99.6%。
OBJECTIVE To design a bioactive metabolite of ebastine, a new anti-allergic drug, ebastine. Methods Benzoyl chloride was used as a starting material to afford the intermediate diphenylbromomethane (4) via acylation, reduction and displacement reactions. The α, α-dimethylbenzene acetic acid was used as the starting material to obtain the intermediate 9; intermediate 4 and intermediate 9 by condensation, hydrolysis reaction to give the desired product. Results and Conclusions The total yield of the target compound was 21.0%. Its structure was confirmed by 1H-NMR and M-S spectra. The purity was 99.6% by HPLC.