LSZ102 - From MedChem to manufacturing process
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
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.