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以文拉法辛为原料,分别以新的脱甲基试剂半胱氨酸钠盐和青霉胺钠盐制备了O-去甲基文拉法辛,收率为86%和82%.一锅中分别完成了半胱氨酸钠盐、青霉胺钠盐的制备与文拉法辛脱甲基反应,简化了操作步骤.最优反应条件为溶剂N-甲基吡咯烷酮,反应温度175℃,产物析晶pH值9.5.

参考文献

[1] Beat T W,Zofingen C H.Methods for Preparing O-Desmethylvenlafaxine:US,20030105358A1[P],2003-06-05.
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[5] Niddamhildelsheim V.Substantially Pure O-Desmethylvenlafaxine and Processes for Preparing Its:WO,2007120923[P],2007-10-25.
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