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以顺丁烯二酸酐和呋喃为起始原料,经Diels-Alder[4+2]缩合反应,制备去甲去氢斑蝥素,同时在去甲去氢斑蝥素分子中引入电负性较大的氧原子、氮原子。去甲去氢斑蝥素经SN2取代、缩合和过氧酸氧化三步反应,合成了5,6-环氧去甲去氢斑蝥素衍生物,去甲去氢斑蝥素经S_N2取代、缩合、过氧酸氧化和取代四步反应,得到5,6-二羟基去甲去氢斑蝥素衍生物。所得化合物均经~1HNMR和ESI-MS确证。
Maleic anhydride and furan as starting materials, the Diels-Alder [4 +2] condensation reaction, preparation of norcantharidin, at the same time in the norcantharidin molecules into the larger electronegativity Oxygen atom, nitrogen atom. N-dehydro-cantharidin by SN2 substitution, condensation and peroxyacid oxidation three-step reaction, synthesis of 5,6-epoxy norcantharidin derivatives, nordic dehydrocatechin S_N2 by substitution, condensation, and Oxidation of oxygen and substitution of four-step reaction to give 5,6-dihydroxy norcantharidin derivatives. The resulting compounds were confirmed by ~ 1HNMR and ESI-MS.