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唑来膦酸属于第三代双膦酸药物,是含氮杂环双膦酸和吡啶双膦酸盐的骨吸收抑制剂。由于具有活性强、毒性低等优点,因而具有良好的应用前景。对唑来膦酸工艺进行了改进,通过加入分散剂解决了膦酸化步骤的固化问题。探索出了一种有效的分散剂,解决了双膦酸类化合物制备过程中膦酸化步骤容易固化结块制约工业化生产的问题,经工业放大生产被证明该改进工艺是可行的,合理的。
Zoledronic acid belongs to the third generation of bisphosphonates and is a bone resorption inhibitor of nitrogen-containing heterocyclic bisphosphonates and pyridine bisphosphonates. Because of its strong activity, low toxicity, which has good application prospects. The zoledronic acid process was improved by adding a dispersant to solve the problem of curing phosphonation step. Explored an effective dispersant to solve the problem that during the preparation of bisphosphonates, the phosphonation step easily cures and blocks the industrialized production, and the industrialized production proves that the improved process is feasible and reasonable.