二膦酸盐去氢胆酰化衍生物的设计、合成及分析

Design,synthesis and analysis of dehydrocholic acid acylation derivatives of bisphosphonates

目的:设计、合成新型结构的二膦酸盐衍生物,并建立其高效液相色谱分析方法。方法:采用活化酯法合成阿仑膦酸及帕米膦酸的去氢胆酸酰胺化衍生物(DHC-BPs),通过IR、MS和NMR确证衍生物结构。采用Cu2+络合法,对衍生物进行HPLC分析。结果:合成的化合物为DHC-BPs,建立的HPLC方法能用于分析所合成的化合物,且具有一定的选择性。结论:DHC-BPs是值得进一步研究的二膦酸盐类衍生物。

OBJECTIVE To design and synthesize novel bisphosphonates derivatives, and to establish the analysis method. METHODS Synthesis of dehydrocholic acid was made acylation derivatives of alendronate acid and pamidronate acid was made by activated ester. The structures of the derivatives were confirmed by IR.MS and NMR. HPLC analysis of the derivatives via compler formathon with Cu2＋ . RESULTS The compounds synthesized were DHC BPs. The HPLC method established ould be used to analyize the derivatives, and the method was demonstrated to be selective. CONCLUSION DHC-BPs are worthy of further study.