Cabazitaxel 1 is an antineoplastic agent belonging to the taxane class and approved for the treatment of hormone-refractory prostate cancer. During the optimization process of cabazitaxel, six related substances were detected using the gradient high-performance liquid chromatography technique. A thorough study was undertaken to identify, prepare, and control these six related substances. The molecular weights were determined by liquid chromatography–mass spectrometry analysis. Using spectroscopic analysis (high-resolution mass spectrometry (HRMS), infrared (IR), and NMR), the structures were determined as an amino alcohol derivative (CRS-1), 7,10-dimethoxy-10-deacetylbaccatin III (CRS-2), an N-formyl-related substance (CRS-3), 7,10,13-trimethoxy-10-deacetylbaccatin III (CRS-4), a DiBOC-related substance (CRS-5), and a process-related intermediate (CRS-6). The mechanistic aspects of the formation, synthesis, and control strategy of the associated substances were examined in detail.

中文翻译：

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卡巴他赛相关物质的大规模合成、表征和控制策略


卡巴他赛 1 是一种属于紫杉烷类的抗肿瘤药，被批准用于治疗激素难治性前列腺癌。在卡巴他赛优化过程中，采用梯度高效液相色谱技术检测 6 种相关物质。对这六种相关物质进行了深入研究。通过液相色谱-质谱分析确定分子量。使用光谱分析（高分辨率质谱 （HRMS）、红外 （IR） 和 NMR），将结构确定为氨基醇衍生物 （CRS-1）、7,10-二甲氧基-10-脱乙酰巴卡丁 III （CRS-2）、N-甲酰相关物质 （CRS-3）、7,10,13-三甲氧基-10-脱乙酰巴卡丁 III （CRS-4）、DiBOC 相关物质 （CRS-5） 和工艺相关中间体 （CRS-6）。详细研究了相关物质的形成、合成和控制策略的机械方面。