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    • 1. 发明授权
    • Method for producing optically active 2-arylpiperazine derivative
    • 光学活性2-芳基哌嗪衍生物的制备方法
    • US08273883B2
    • 2012-09-25
    • US12449460
    • 2008-02-05
    • Masatoshi OhnukiAkira NishiyamaMasaru Mitsuda
    • Masatoshi OhnukiAkira NishiyamaMasaru Mitsuda
    • C07D241/04C07D295/00
    • C07B53/00C07D241/04
    • The objective of the present invention is to produce an optically active 2-arylpiperazine derivative useful as a synthetic intermediate for pharmaceutical products and agricultural chemicals from inexpensive and readily available starting material by an industrially practicable method. The objective can be accomplished by treating an optically active substituted aminodiol derivative produced from an optically active styrene oxide derivative with a sulfonating agent in the presence of a base, and then reacting an amine compound to obtain the 2-arylpiperazine derivative. Especially, an optically active 1-unsubstituted-2-arylpiperazine derivative can be produced by treating an optically active 1-allyl-2-arylpiperazine derivative with water in the presence of a transition metal catalyst for deallylation.
    • 本发明的目的是通过工业上可行的方法从便宜且容易获得的原料制备用作药物产品和农药的合成中间体的光学活性2-芳基哌嗪衍生物。 该目的可以通过在碱的存在下用磺化剂处理由光学活性苯乙烯氧化物衍生物产生的光学活性取代的氨基二醇衍生物,然后使胺化合物反应得到2-芳基哌嗪衍生物来实现。 特别地,光学活性的1-未取代-2-芳基哌嗪衍生物可以通过在过渡金属催化剂的存在下用水处理光学活性的1-烯丙基-2-芳基哌嗪衍生物来进行脱气。