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目的新法合成新型抗肿瘤树化胺基甾醇类似物6β-丁胺基胆甾-3β,5α-二醇。方法以胆固醇为原料,3β,5α-二羟基胆甾-6-酮为关键中间体,亚胺化-还原为关键步骤,经5步反应合成6β-丁胺基胆甾-3β,5α-二醇。结果以62%的总收率合成了目标化合物,其结构与实测MS(476)、HRMS(476.4465)、[α]2D5(-57.0°)、IR(3387)、1HNMR[2.67～2.61(1H,m,6α-H)]、13CNMR和元素分析一致。结论以本法合成6β-丁胺基胆甾-3β,5α-二醇,原料廉价易得、总收率高、易于工业化。
Aim To synthesize 6β-butylamidocholesterol-3β, 5α-diol which is a novel anti-tumor epinephrine phytosterol analogue. Methods Cholesterol as raw material, 3β, 5α-dihydroxycholesta-6-one as the key intermediate, imidization - reduction as the key step, synthesis of 6β-butylamidocholesterol-3β, 5α- alcohol. Results The target compound was synthesized in 62% overall yield. Its structure was similar to that of MS (476), HRMS (476.4465), [α] 2D5 (-57.0 °), IR (3387), 1HNMR [2.67-2.61 m, 6α-H)], 13CNMR consistent with elemental analysis. Conclusion 6β-butylamidocholesterol-3β, 5α-diol is synthesized by this method. The raw materials are cheap and easily available, the total yield is high, and industrialization is easy.