【摘要】 目的 对他泽司他（tazemetostat）的合成工艺进行优化。方法 以2-甲基-3-硝基-5-溴苯甲酸甲酯为原料，经氢化还原、两次还原胺化、水解、酸胺缩合、镍催化Suzuki偶联6步反应得到目标物tazemetostat。结果与结论经¹H-NMR、¹³C-NMR谱表征确证目标物的结构，总收率为28.88%,纯度达99.2%（HPLC法）。该方法操作简单，Suzuki偶联反应中不使用重金属钯，产物中无重金属钯残留，绿色安全。更多还原

【Abstract】 To improve the synthetic process of tazemetostat, the target product was obtained from methyl 5-bromo-2-methyl-3-nitrobenzoate via a six-step process including hydrogenation reduction, twice reductive amination, hydrolysis, amidation formation, and Ni-catalyzed Suzuki coupling.The target product was characterized by ¹H-NMR and ¹³C-NMR,with a total yield of 28.88% and a purity of 99.2%（HPLC method）.The method is simple to operate, green and safe, and has no residual palladium in the product.更多还原