利索-全球专利检索

  1. 登录
  2. 注册
发明公开
CN106188193A (2`R)-2`-脱氧-2`-卤代-2`-甲基脲苷衍生物、其制备方法和用途 无效 - 撤回

(2`R)-2`-脱氧-2`-卤代-2`-甲基脲苷衍生物、其制备方法和用途
摘要：
本发明公开了式I化合物及其制备方法和中间体；式I化合物用于制备治疗病毒感染疾病药物的用途；式I化合物在制备索氟布韦及其类似物中的用途以及使用式I化合物制备索氟布韦及其类似物的方法。本发明要求保护的方法通过设计新的反应路线，避免了磷酰化反应中使用叔丁基氯化镁引起的副反应，减少了生成的杂质，降低了后续的纯化工序的难度。而且经试验证明，本发明要求保护的方法，反应条件温和，易于操作，收率高，得到的产物质量稳定，纯度高，可以进行工业规模放大生产。
摘要（英）：

The present invention discloses a compound represented by a formula I, a preparation method and an intermediate thereof, uses of the compound represented by the formula I in preparation of drugs for treatment of viral infection diseases, uses of the compound represented by the formula I in preparation of sofosbuvir and analogs thereof, and a method for preparing the sofosbuvir and the analogs thereof by using the compound represented by the formula I. According to the method of the present invention, the new reaction route is designed, such that the side reaction caused by the use of tert-butyl magnesium chloride in the phosphorylation reaction is avoided, the generated impurity is reduced, and the difficulty of the subsequent purification process is reduced. According to the present invention, the test results prove that the method has characteristics of mild reaction conditions, easy operation, high yield, stable product quality and high product purity, and can be used for industrial scale enlargement production. The formula I is defined in the specification.

0/0