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    LSZ102 - From MedChem to manufacturing process

    发布时间:2025-09-15

    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:2025923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.

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