抗丙肝药物faldaprevir的合成

Synthesis of an anti-hepatitis C drug,faldaprevir

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.