An Effective and Convenient Process for the Preparation of Ticagrelor: Optimized by Response Surface Methodology and One-Pot Reaction
- Авторы: Wang L.1, Liu J.1
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Учреждения:
- Department of Pharmaceutical Engineering, Qingdao University of Science & Technology
- Выпуск: Том 52, № 10 (2019)
- Страницы: 813-819
- Раздел: Molecular-Biological Problems of Drug Design and Mechanism of Drug Action
- URL: https://journals.rcsi.science/0091-150X/article/view/245486
- DOI: https://doi.org/10.1007/s11094-019-1906-x
- ID: 245486
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Аннотация
An effective and convenient process for the preparation of ticagrelor (1), an antiplatelet drug, has been developed. The synthesis of 1 is a four-step reaction. Each reaction step was optimized individually to develop a scalable and industrial friendly process. The critical step to prepare intermediate 5 was optimized using the response surface methodology. One-pot reaction was used to telescope the next three steps, resulting in 75% overall yield in comparison to the initial 63% yield obtained from the stepwise isolation process. The feasibility and consistency of the improved process was verified by pilot-scale test.
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Li-hong Wang
Department of Pharmaceutical Engineering, Qingdao University of Science & Technology
Автор, ответственный за переписку.
Email: wanglihong1230@163.com
Китай, 53 Zhengzhou Road, Qingdao, Shandong province, 266000
Jun-hong Liu
Department of Pharmaceutical Engineering, Qingdao University of Science & Technology
Email: wanglihong1230@163.com
Китай, 53 Zhengzhou Road, Qingdao, Shandong province, 266000