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    • 3. 发明申请
    • METHODS FOR SYNTHESIZING SUBSTITUTED TETRACYCLINE COMPOUNDS
    • 用于合成取代的四氢化合物化合物的方法
    • WO2009009042A1
    • 2009-01-15
    • PCT/US2008/008355
    • 2008-07-07
    • PARATEK PHARMACEUTICALS, INC.SEYEDI, FarzanehWARCHOL, TadeuszGRIER, Mark
    • SEYEDI, FarzanehWARCHOL, TadeuszGRIER, Mark
    • C07C237/26
    • C07C231/12C07C2603/44C07C237/26
    • Methods for synthesizing a carboxaldehyde substituted tetracycline compound comprising reacting a tetracycline reactive intermediate under appropriate conditions with carbon monoxide, a palladium catalyst, a phosphine ligand, a silane and a base, such that said carboxaldehyde substituted tetracycline compound is synthesized. The palladium catalyst is chosen from PdCl2 (tBu2PhP)2 dichlorobis (di-tert-butylphenylphosphine palladium (II)] or PdCl2 (DPEPhos) [bis (diphenylphosphinophenyl) ether palladium (II) chloride]. The tetracycline reactive intermediate contains moieties selected from halogens and triflates. Methods of synthesizing a substituted tetracycline compound comprising reacting the carboxaldehyde substituted tetracycline compound under palladium catalyzed coupling conditions, hydrogenolysis conditions or reductive amination conditions.
    • 合成羧甲醛取代的四环素化合物的方法,包括在合适的条件下使四环素反应性中间体与一氧化碳,钯催化剂,膦配体,硅烷和碱反应,使得所述甲醛取代的四环素化合物合成。 钯催化剂选自PdCl2(tBu2PhP)2二氯双(二叔丁基苯基膦钯(II)]或PdCl 2(DPEPhos)[双(二苯基膦基苯基)醚氯化钯(II)],四环素反应性中间体包含选自卤素 合成取代的四环素化合物的方法,包括在钯催化的偶联条件下,氢解条件或还原胺化条件下使羧醛取代的四环素化合物反应。