From a careful analysis of the recent literature, it seems clear that many transition-metal-catalyzed processes used in API synthesis are developed without resorting to any kind of kinetic analysis. Even acknowledging that some of these processes were developed for early development projects and did not need to be thoroughly optimized, the lack of kinetic work is surprising. This Perspective suggests that, in addition to the utilization of modern technologies such as high-throughput experimentation (HTE) and classical optimization tools such as Design of Experiments (DOE), a modest level of kinetic analysis is necessary to develop truly effective catalytic reactions. We offer some basic theoretical considerations and suggest some rather simple tools which can be employed to integrate kinetic analysis of catalytic steps into API development.

中文翻译：

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如何在制药行业开展有机金属催化反应

通过对近期文献的仔细分析，很明显 API 合成中使用的许多过渡金属催化工艺都是在不借助任何类型的动力学分析的情况下开发的。即使承认其中一些过程是为早期开发项目开发的并且不需要彻底优化，但缺乏动力工作仍然令人惊讶。该观点表明，除了利用高通量实验 (HTE) 等现代技术和实验设计 (DOE) 等经典优化工具外，还需要适度的动力学分析来开发真正有效的催化反应。我们提供了一些基本的理论考虑，并提出了一些相当简单的工具，可用于将催化步骤的动力学分析集成到 API 开发中。