An improved synthetic method for the gram-scale preparation of SAR407899 as ROCK inhibitor: A tool for an undergraduate laboratory course

As a novel Rho-associated protein kinase (ROCK) inhibitor, SAR407899 exhibits significant efficacy in the fields of antihypertension, vasodilation, and improvement of erectile function. Due to its potent bioactivity and unique fragment, SAR407899 is widely recognized as an important chemical tool in the development of novel ROCK inhibitors. Until now, only one synthetic method has been reported, which exhibits several drawbacks such as high-temperature reaction and usage of explosive and toxic materials. Consequently, it is of great significance to optimize the synthetic process of SAR407899 . In this paper, we report an alternative, safe, and cost-efficient protocol for the synthesis of the ROCK inhibitor SAR407899 , which obviates the use of hazardous and costly reagents. Developed in innovative research training courses, this method exemplifies the successful integration of research-oriented education with practical synthetic chemistry. The application of a complete synthetic process of a drug in undergraduate laboratory courses represents an exploration of experimental teaching in college. The results verified that the teaching approach is suitable for undergraduate experiment courses. It not only developed the students’ experimental skills but also motivated their research interest.