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    • 7. 发明申请
    • Process for halomethyl ethers of hydroxyiminomethyl quaternary pyridinium salts
    • 羟基亚氨基甲基季吡啶盐的卤代甲基醚的方法
    • US20060183777A1
    • 2006-08-17
    • US11133740
    • 2005-05-19
    • Der-Shing HuangGeorge GettysOlivier DapremontAslam Malik
    • Der-Shing HuangGeorge GettysOlivier DapremontAslam Malik
    • A61K31/44
    • C07D213/53C07D213/81
    • A halide salt of a 1-(hydroxyiminomethyl-1-pyridino)-3-(halomethyl)-2-oxapropane is prepared by adding a pyridinealdoxime to a bis-halomethylether in such a manner that the bis-halomethylether is maintained in excess throughout the addition. This procedure produces the halide salt of a 1-(hydroxyiminomethyl-1-pyridino)-3-(halomethyl)-2-oxapropane in high yield and purity, which facilitates its use as an intermediate in the manufacture of an asymmetrically substituted 1,3-di (1-pyridino)-2-oxapropane, a class of compounds that are generally useful antidotes to various toxic agents. A prominent member of the class is the dimethylsulfonate salt of 1-(2-hydroxyiminomethyl-1-pyridino)-3-(4-carbamoyl-1-pyridino)-2-oxapropane. The use of mercaptoalkyl-functionalized polymers is disclosed as a preferred metal ion scavenger for a final purification step in the manufacture of these compounds.
    • 通过向双卤代甲醚中加入吡啶醛肟制备1-(羟基亚氨基甲基-1-吡啶基)-3-(卤代甲基)-2-氧杂丙烷的卤化物盐,使双 - 卤代甲醚在整个过程中保持过量 加成。 该方法以高产率和纯度产生1-(羟基亚氨基甲基-1-吡啶基)-3-(卤代甲基)-2-氧杂丙烷的卤化物盐,这有助于其用作制备不对称取代的1,3 -di(1-吡啶基)-2-氧杂丙烷,一类通常用于各种毒性剂的解毒剂的化合物。 该类的突出成员是1-(2-羟基亚氨基甲基-1-吡啶基)-3-(4-氨基甲酰基-1-吡啶基)-2-氧杂丙烷的二甲基磺酸盐。 公开了使用巯基烷基官能化聚合物作为优选的金属离子清除剂,用于制造这些化合物的最终纯化步骤。