抗丙肝药物faldaprevir的合成  

Synthesis of an anti-hepatitis C drug,faldaprevir

作　　者：胡宏亮[1] 朱雪焱[1] 袁哲东[1] 俞雄 黄雨[1] 

机构地区：[1]上海医药工业研究院,上海200437 [2]中国医药工业研究总院,上海200040

出　　处：《中国新药杂志》2015年第4期452-456,共5页Chinese Journal of New Drugs

摘　　要：目的:抗丙肝新药faldaprevir的合成。方法:以1-(2-氨基-3-溴-4-甲氧基苯基)乙酮为原料经缩合,环化,取代反应,芳香亲核取代,氨基酸缩合和水解反应制得faldaprevir。结果:最终产物faldaprevir经1H-NMR和ESI-MS确证化学结构正确。纯度经HPLC检测可达99.9%,路线总收率达34.8%。结论:该合成工艺操作简单,条件温和,产物纯度好,收率高,适合用于工业化生产。Objective： To synthesize the anti-hepatitis C drug, faldaprevir. Methods： Using 1-（2-Amino- 3-bromo-4-methoxyphenyl） ethanone as start material, the synthesis consisted of one condensation step, one quinolone cyclic condensation step, two nucleophilic aromatic substitution steps, one amide bond formations step and one hydrolysis step of methyl ester. Results： The verified target material faldaprevir was synthesized with a total yield of 34.8% , and the purity was 99.9% as determined by HPLC. Conclusion： With high purity and yield, this synthetic process is easy to operate in a mild condition, h is suitable for further industrial production.

关 键 词：丙型肝炎 faldaprevir 合成 

分 类 号：R914.5[医药卫生—药物化学]