CAS: 509-71-7; Dihydroheroine

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二乙酰基吗啡 Diamorphine 561-27-3

📜二乙酰基吗啡置于5%-Palladium/activated Carbon,氢气体系中,用 乙醇,苯 作为反应溶剂,以90%的收率获得产物双醋氢吗啡
参考文献:吗啡苯甲酸酯及其衍生物的制备
标题:吗啡苯甲酸酯及其衍生物的制备
摘要:摘要持续镇痛对于遭受长效疼痛的患者至关重要.吗啡的酯衍生物可以增强吗啡的亲脂性.因此,其透皮递送及其作用持续时间也增加了.因此,二十一3-O-,6-O-和14-O合成了吗啡的苯甲酸酯及其衍生物,以阐明适用于这些广泛使用的化合物进行酯化的不同合成方法.schotten-Baumann反应与碳酸氢钠,三乙胺或吡啶在二氯甲烷或1,2-二氯乙烷中的溶剂一起应用.主要在叔醇的情况下也成功地利用了4-二甲基氨基吡啶催化剂的存在.还提出了通过不含副产物的二乙酰基吗啡合成二氢吗啡的新方法.通过1 H核磁共振(NMR),13 C NMR,高分辨率质谱(hrms)和电子电离质谱(ei-Ms)阐明了所有合成化合物的结构.日志 D通过反相高效液相色谱(HPLC)-ms方法测定合成化合物的(ph 7.4)值,并提供计算出的水解速率常数.合成的苯甲酸酯是母体吗啡的潜在前药,具有增强的亲脂性,这些衍生物也可用于经皮给药,作为预期的长效麻醉镇痛药.
DOI:10.1007/s00706-012-0803-8

专利信息

专利号:US-5900227-A
优先权日:1996-06-17
标题 :Multicyclic nitrone spin trapping compositions
发明人：JANZEN EDWARD G; SANKURATRI NAGARAJU
权利人:OKLAHOMA MED RES FOUND
摘要:Multicyclic nitrone spin trapping compounds capable of forming stable free radical spin adducts are provided as well as methods for their synthesis. The multicyclic nitrone spin trapping compounds can be reacted with a free radical, such as a hydroxy or hydroperoxy radical, in solution to form a spin adduct which is stable and readily detectable by electron paramagnetic resonance (EPR) spectroscopy. The multicyclic nitrone spin traps can be used to detect free radicals in a sample such as a biological system. In one embodiment, the spin trapping compound, 1,3,3-trimethyl-6-azabicyclo-[3.2.1]oct-6-ene-N-oxide ('TRAZON') is provided, as well as methods for the synthesis of TRAZON and of modified forms of TRAZON. TRAZON can react with a wide range of different free radicals in solution to form free radical spin adducts which are readily detectable by EPR.