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Development of a Kilogram-Scale Synthesis of a Novel Anti-HCV Agent, CH4930808
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2018-01-29 00:00:00 , DOI: 10.1021/acs.oprd.7b00383
Tsuyoshi Haneishi 1 , Yoshiaki Kato 2 , Hiroshi Fukuda 1 , Tomoyuki Shimamura 2 , Takemi Tanokura 2 , Akira Hiraide 2 , Kaichiro Koyama 2 , Masato Fudesaka 2 , Kenji Maeda 2 , Nobuyuki Nakata 2 , Masahiro Nagase 2 , Takahiko Yabuzaki 2 , Hiroaki Takao 2 , Masaharu Kigawa 2 , Hitoshi Shimizu 2 , Makoto Shimizu 3
Affiliation  

Herein, we report the kilogram-scale synthesis of CH4930808 (1), a novel anti-hepatitis C virus agent. While pursuing improved productivity using many through-process strategies, we conducted scrupulous impurity control. Finally, we successfully developed a practical and scalable process for the synthesis of (1·1.5Na·2.5H2O), by which we prepared 3.28 kg of the active pharmaceutical ingredient for clinical studies.

中文翻译:

公斤级合成新型抗HCV药物CH4930808的开发

在此,我们报道了新型抗丙型肝炎病毒药物CH4930808(1)的千克级合成。在使用许多贯穿过程的策略追求提高生产率的同时,我们进行了严格的杂质控制。最后,我们成功开发了一种实用且可扩展的合成(1 ·1.5Na·2.5H 2 O)的方法,由此制备了3.28千克的活性药物成分用于临床研究。
更新日期:2018-01-29
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