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    Process for exchanging functional groups by halogen-metal exchange reaction
    2.
    发明授权
    Process for exchanging functional groups by halogen-metal exchange reaction 失效
    通过卤素 - 金属交换反应交换官能团的方法

    公开(公告)号：US07439535B2

    公开(公告)日：2008-10-21

    申请号：US11077292

    申请日：2005-03-11

    申请人： Takehiko Iida ,  Toshihiro Wada ,  Toshiaki Mase

    发明人： Takehiko Iida ,  Toshihiro Wada ,  Toshiaki Mase

    IPC分类号： C07F3/02

    CPC分类号： C07D213/84 ,  C07C45/004 ,  C07C45/45 ,  C07D213/61 ,  C07D333/28 ,  C07F3/02 ,  C07F7/0827 ,  C07C47/55

    摘要： A method by which a halogen atom of a halogen compound can be efficiently replaced with an electrophilic group.Also provided are: a reagent for converting a functional group through a halogen-metal exchange reaction, characterized by comprising either a mixture of a magnesium compound represented by the formula R1—Mg—X (I) (wherein R1 represents a halogen atom or an optionally substituted hydrocarbon residue; and X1 represents a halogen atom) and an organolithium compound represented by the formula R2—Li (II)(wherein R2 represents an optionally substituted hydrocarbon residue) or a product of the reaction of the magnesium compound with the organolithium compound; and a process for producing with the reagent a compound in which a halogen atom of a halogen compound has been replaced with an electrophilic group.

    摘要翻译： 可以用亲电子基团有效地代替卤素化合物的卤素原子的方法。 还提供：用于通过卤素 - 金属交换反应转化官能团的试剂，其特征在于包含由式R 1 -Mg-X（I）表示的镁化合物的混合物（ 其中R 1表示卤素原子或任选取代的烃残基; X 1表示卤素原子）和由式R 2表示的有机锂化合物， （II）（其中R 2表示任选取代的烃残基）或镁化合物与有机锂化合物的反应的产物; 以及用该试剂制备其中卤素化合物的卤素原子已被亲电子基团取代的化合物的方法。

    Method for producing thioether compound
    6.
    发明授权
    Method for producing thioether compound 失效
    硫醚化合物的制备方法

    公开(公告)号：US07683218B2

    公开(公告)日：2010-03-23

    申请号：US11664663

    申请日：2005-10-07

    申请人： Takahiro Itoh ,  Toshiaki Mase ,  Atsushi Akao

    发明人： Takahiro Itoh ,  Toshiaki Mase ,  Atsushi Akao

    IPC分类号： C07C319/16

    CPC分类号： C07D213/32 ,  B01J31/2457 ,  B01J2531/824 ,  C07C319/14 ,  C07C2601/14 ,  C07D209/08 ,  C07D213/70 ,  C07F17/02 ,  C07C321/28 ,  C07C321/30 ,  C07C323/09 ,  C07C323/16 ,  C07C323/20 ,  C07C323/22 ,  C07C323/52

    摘要： Disclosed is an efficient and widely-applicable method for commercially producing a thioether compound or a thiol compound which is useful as a pharmaceutical compound or a production intermediate of it. Specifically disclosed is a method for producing a thioether compound represented by the general formula [I] below or a salt thereof. This method is characterized in that a compound represented by the following general formula [III]: [III] (wherein X represents a bromine atom, a chlorine atom or a trifluoromethylsulfonyloxy group, and ring A represents an aryl group or a heteroaryl ring group) or a salt thereof is reacted with a thiol compound represented by the following general formula [II]: [II] or a salt thereof in the presence of a palladium compound such as Pd2(dba)3, a base such as i-Pr2NEt and a phosphorus compound represented by the following formula [AA].

    摘要翻译： 公开了用于商业生产硫醚化合物或硫醇化合物的有效和广泛应用的方法，其可用作药物化合物或其制备中间体。 具体公开了由下述通式[I]表示的硫醚化合物或其盐的制备方法。 该方法的特征在于由以下通式[III]表示的化合物：[III]（其中X表示溴原子，氯原子或三氟甲基磺酰氧基，环A表示芳基或杂芳基环基） 或其盐与下列通式[II]表示的硫醇化合物：[II]或其盐在钯化合物如Pd 2（dba）3，诸如i-Pr 2 N Et的碱和 由下式[AA]表示的磷化合物。

    Process for producing indolopyrrolocarbazole derivative
    7.
    发明申请
    Process for producing indolopyrrolocarbazole derivative 审中-公开
    吲哚吡咯并咔唑衍生物的制备方法

    公开(公告)号：US20070197796A1

    公开(公告)日：2007-08-23

    申请号：US11597770

    申请日：2005-05-26

    申请人： Takehiko Iida ,  Shouichi Hiraga ,  Akihiro Takezawa ,  Toshiaki Mase

    发明人： Takehiko Iida ,  Shouichi Hiraga ,  Akihiro Takezawa ,  Toshiaki Mase

    IPC分类号： C07H19/00

    CPC分类号： C07D403/14 ,  C07D487/14 ,  C07H19/23 ,  Y02P20/55

    摘要： The present invention relates to an industrially preferable process for producing an indolopyrrolocarbazole derivative represented by the formula (I): or a pharmaceutically acceptable salt thereof, which is useful as an anti-cancer agent. The above process comprises treating a compound represented by the formula (V): or a pharmaceutically acceptable salt thereof, a solvate thereof or a salt thereof, with a base in an inert solvent, followed by treatment with an acid, and further treating the resulting reaction solution with a base in an inert solvent and subsequently with an acid, and then reacting the resulting compound with an acid addition salt of hydrazine diol in the presence of an acid scavenger, followed by removal of protecting group(s) from the resulting compound.

    摘要翻译： 本发明涉及一种工业上优选的用于制备可用作抗癌剂的式（I）表示的吲哚并吡咯并唑衍生物或其药学上可接受的盐的方法。 上述方法包括在惰性溶剂中用碱处理式（V）表示的化合物或其药学上可接受的盐，其溶剂合物或其盐，然后用酸处理，并进一步处理所得 反应溶液与碱在惰性溶剂中随后与酸反应，然后在酸清除剂存在下使所得化合物与肼二酸的酸加成盐反应，然后从所得化合物中除去保护基 。