All Categories (1-3 of 3)

1. Development of a Continuous Flow Process for the Efficient Preparation of Anti-Tuberculosis-Specific Drug TBAJ-876

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   24 Apr 2024 | Contributor(s):: Gao, Feng, Zhang, Guowei, Gu, Wenting, Zhang, Zhenfeng, Liu, Zhiqing, Zhang, Wanbin, Li, Jing

   Previously, the first asymmetric synthesis of anti-tuberculosis agent TBAJ-876 had been successfully achieved using a synergistic Li/Li catalysis approach, yielding excellent results on a 5 g scale. However, scaling up the process presents significant challenges due to its poor repeatability and...

2. Mechanistic investigation of a Ru-catalyzed direct asymmetric reductive amination reaction for a batch or continuous process scale-up: an industrial perspective

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   09 Jun 2023 | Contributor(s):: Changi, SM, Yokozawa, TYamamoto, T, Nakajima, H, Embry, MC, Vaid, R, Luciani, CV, Wong, SW, Johnson, M, Moher, ED

   A comprehensive assessment of a Ru-catalyzed direct asymmetric reductive amination (DARA) reaction for producing an intermediate for an active pharmaceutical ingredient (API) was carried out. Experiments were conducted to investigate the impact of process parameters (such as reaction temperature,...

3. Continuous flow asymmetric synthesis of chiral active pharmaceutical ingredients and their advanced intermediates

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   09 Jun 2023 | Contributor(s):: Otvos, SB, Kappe, CO

   Catalytic enantioselective transformations provide well-established and direct access to stereogenic synthons that are broadly distributed among active pharmaceutical ingredients (APIs). These reactions have been demonstrated to benefit considerably from the merits of continuous processing and...