题  目：LSZ102 - From MedChem to manufacturing process

报告人：Dr. Michael Parmentier

        Chemical & Analytical Development, 

        Novartis Pharma AG,Basel,Switzerland

主持人：马大为 院士

时  间：2025年9月23日（星期二）下午 14:30 - 16:00

地  点：君谋楼二楼 第一会议室

欢迎听讲！

【Abstract】

The process development for the selective estrogen receptor degrader (SERD) candidate LSZ102 is outlined, emphasizing the transition from medicinal chemistry synthesis to large-scale production. The synthesis was significantly enhanced by revising the initial disconnection strategy, which led to improvements in overall yield, the elimination of chromatographic purifications, and a reduction in the number of steps. Additionally, an alternative micellar chemistry process for the crucial C-H functionalization step is introduced, which notably decreases a critical impurity level. Special consideration was given to the scalability of reaction conditions, environmental impact, and safety.