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    • 2. 发明申请
    • PROCESS FOR PRODUCING ACID-ADDITION SALT OF Z-ISOMER OF TRIPHENYLETHYLENE COMPOUND
    • 生产三苯乙烯化合物的Z-异构体酸的添加剂的方法
    • WO1995011879A1
    • 1995-05-04
    • PCT/JP1994001782
    • 1994-10-25
    • TAIHO PHARMACEUTICAL CO., LTD.SHINOZAKI, FumihikoNAGASAWA, HiroshiMARUHASHI, Kazuo
    • TAIHO PHARMACEUTICAL CO., LTD.
    • C07C217/18
    • C07C217/18C07C213/08
    • A process for producing an acid-addition salt of a Z-isomer of a compound represented by general formula (I) (wherein R and R represent each lower alkyl, or are combined together with the nitrogen atom to which they are bonded to thereby form a nitrogenous heterocyclic group which may bear other heteroatom(s); R and R represent each hydrogen, lower alkyl, hydroxy, lower alkoxy, lower alkylcarbonyloxy, arylcarbonyloxy wherein the benzene ring may be substituted by one or two groups selected from among lower alkyl, lower alkoxy, halogen and cyano, benzylcarbonyloxy, mono- or di(lower alkyl)aminocarbonyloxy, or mono- or di(aryl)aminocarbonyloxy; R represents lower alkyl or halogen; and n represents 1 to 6), which process comprises heating an E-isomer of a compound represented by general formula (I) or an acid-addition salt thereof, either alone or as a mixture thereof with a Z-isomer of a comound represented by general formula (I) or an acid-addition salt thereof, in an organic solvent containing hydrobromic acid.
    • 一种制备通式(I)表示的化合物的Z-异构体的酸加成盐的方法(其中R 1和R 2代表每个低级烷基,或与氮原子相结合 它们被键合从而形成可含有其它杂原子的含氮杂环基; R 3和R 4代表各自的氢,低级烷基,羟基,低级烷氧基,低级烷基羰基氧基,芳基羰基氧基,其中苯环可以是 被一个或两个选自低级烷基,低级烷氧基,卤素和氰基的基团取代,苄基羰基氧基,一或二(低级烷基)氨基羰基氧基或一或二(芳基)氨基羰基氧基; R 5表示低级烷基或卤素 ; n表示1至6),该方法包括将通式(I)表示的化合物的E-异构体或其酸加成盐单独或作为其与组合的Z-异构体的混合物 由通式(I)表示的化合物或其酸加成盐 含有氢溴酸的厌氧溶剂。
    • 9. 发明授权
    • Process for preparing acid addition salt of Z-isomer of
triphenylethylene compound
    • 制备三苯乙烯化合物Z-异构体的酸加成盐的方法
    • US5565611A
    • 1996-10-15
    • US446736
    • 1995-06-06
    • Shinozaki FumihikoNagasawa HiroshiMaruhashi Kazuo
    • Shinozaki FumihikoNagasawa HiroshiMaruhashi Kazuo
    • C07C213/08C07C217/18C07C213/10
    • C07C217/18C07C213/08
    • The present invention provides a process for preparing an acid addition salt of the Z-isomer of a compound of the formula ##STR1## wherein R.sup.1 and R.sup.2 represent a lower alkyl group, or taken together with the nitrogen atom to which they are attached, form a nitrogen-containing heterocyclic group optionally containing other hetero atom or atoms; R.sup.3 and R.sup.4 represent H, a lower alkyl group, OH, a lower alkoxy group, a lower alkylcarbonyloxy group, an arylcarbonyloxy group optionally substituted with 1-2 substituents selected from lower alkyl, lower alkoxy, halo and CN on the benzene ring, a benzylcarbonyloxy group, a mono- or di(lower alkyl)aminocarbonyloxy group or a mono- or di(aryl)aminocarbonyloxy group; R.sup.5 represents a lower alkyl group or halo; and n represents 1-6, characterized in that the E-isomer of the compound of the formula (I) or its acid addition salt, singly or in admixture with the Z-isomer or its acid addition salt, is heated in an organic solvent containing hydrobromic acid.
    • 本发明提供了制备式(I)化合物的Z-异构体的酸加成盐的方法,其中R 1和R 2表示低级烷基,或与它们所在的氮原子一起 形成任选含有其它杂原子或原子的含氮杂环基; R3和R4表示H,低级烷基,OH,低级烷氧基,低级烷基羰氧基,任选被选自苯环上的选自低级烷基,低级烷氧基,卤素和CN的1-2个取代基取代的芳羰基氧基, 一或二(低级烷基)氨基羰基氧基或一或二(芳基)氨基羰基氧基; R5表示低级烷基或卤素; 并且n表示1-6,其特征在于式(I)化合物的E-异构体或其酸加成盐单独或与Z-异构体或其酸加成盐混合,在有机溶剂中加热 含氢溴酸。