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    PROCESS FOR PREPARING ITOPRIDE HYDROCHLORIDE
    92.
    发明申请
    PROCESS FOR PREPARING ITOPRIDE HYDROCHLORIDE 审中-公开
    制备氯吡格雷的方法

    公开(公告)号：WO2006051079A1

    公开(公告)日：2006-05-18

    申请号：PCT/EP2005/055839

    申请日：2005-11-09

    Applicant: ERREGIERRE S.p.A. ,  FERRARI, Massimo ,  BONALDI, Matteo

    Inventor： FERRARI, Massimo ,  BONALDI, Matteo

    IPC: C07C231/10 ,  C07C235/48 ,  C07C235/60

    CPC classification number: C07C235/48

    Abstract: Process for preparing itopride hydrochloride comprising: a) Reacting 4-hydroxybenzaldehyde with 2-dimethylaminoethyl chloride in the 5 presence of a weak inorganic base to obtain 4-(2-dimethylaminoethoxy)- benzaldehyde, b) Reacting 4-(2-dimethylaminoethoxy)-benzaldehyde with hydroxylamine hydrochloride in an acid environment to obtain 4-(2-dimethylaminoethoxy)- benzaldoxime hydrochloride, 10 c) Reacting of 4-(2-dimethylaminoethoxy)-benzaldoxime hydrochloride in the presence a reducing agent to 4-(2-dimethylaminoethoxy)-benzylamine, d) Reacting 4-(2-dimethylaminoethoxy)-benzylamine with veratric acid chloride in the presence of a tertiary amine to obtain itopride, e) Salifying itopride with hydrochloric acid to obtain itopride hydrochloride, 15 characterized in that the reducing agent employed in step (c) is powdered zinc.

    Abstract translation: 制备伊曲肽盐酸盐的方法包括：a）在弱无机碱的存在下，用2-二甲基氨基乙基氯反应4-羟基苯甲醛，得到4-（2-二甲基氨基乙氧基） - 苯甲醛，b）使4-（2-二甲基氨基乙氧基） 苯甲醛与盐酸羟胺在酸性环境下反应，得到4-（2-二甲基氨基乙氧基） - 苯甲醛肟盐酸盐，10℃）在还原剂存在下将4-（2-二甲基氨基乙氧基） - 苯甲醛肟盐酸盐反应至4-（2-二甲基氨基乙氧基） - 苄胺，d）在叔胺存在下，用叔油酰氯反应4-（2-二甲基氨基乙氧基） - 苄基胺，得到噻吗化合物，e）用盐酸酸化西来肽，得到盐酸伊坡必利，其特征在于所用还原剂 在步骤（c）中是锌粉。

    ASYMMETRIC UREA COMPOUND AND PROCESS FOR PRODUCING ASYMMETRIC COMPOUND BY ASYMMETRIC CONJUGATE ADDITION REACTION WITH THE SAME AS CATALYST
    93.
    发明申请
    ASYMMETRIC UREA COMPOUND AND PROCESS FOR PRODUCING ASYMMETRIC COMPOUND BY ASYMMETRIC CONJUGATE ADDITION REACTION WITH THE SAME AS CATALYST 审中-公开
    不对称尿素化合物和不对称化合物的生产方法与不同反应物的相容性反应与催化剂

    公开(公告)号：WO2005000803A8

    公开(公告)日：2005-05-12

    申请号：PCT/JP2004009350

    申请日：2004-06-25

    Applicant: SUMITOMO CHEMICAL CO ,  TAKEMOTO YOSHIJI

    Inventor： TAKEMOTO YOSHIJI

    IPC: C07C201/12 ,  C07C205/51 ,  C07C205/53 ,  C07C205/55 ,  C07C231/10 ,  C07C235/78 ,  C07C269/06 ,  C07C271/22 ,  C07C275/30 ,  C07C335/16 ,  C07C335/18 ,  C07D20060101 ,  C07D209/08 ,  C07D209/56

    CPC classification number: C07C335/16 ,  C07B2200/07 ,  C07C205/51 ,  C07C205/53 ,  C07C205/55 ,  C07C269/06 ,  C07C275/30 ,  C07C335/18 ,  C07C2601/14 ,  C07C2602/10 ,  C07D209/08 ,  C07C271/22

    Abstract: A process for producing an asymmetric compound (IV), characterized by causing a compound (II) to add a nucleophilic reagent (III) through conjugate addition in the presence of an asymmetric urea compound (I). Also provided is a nonmetallic asymmetric catalyst capable of realizing asymmetric conjugate addition reaction which attain high yield and are highly stereoselective. The process is an advantageous process for producing an asymmetric compound by an asymmetric conjugate addition reaction in which the catalyst is used. [In the formulae, X represents oxygen or sulfur; C*, C**, and C*** each indicates asymmetric carbon; R , R , R , R , R , R , and R each represents optionally substituted lower alkyl, etc., provided that, for example, R and R may be bonded to each other to form an optionally substituted homocycle, etc.; R represents optionally substituted aryl, etc.; R and R each represents hydrogen, etc.; Nu represents -CR (COR )(COR ) (wherein R , R , and R each represents optionally substituted lower alkyl, etc.), etc.; and EWG represents an electron-withdrawing group.]

    Abstract translation: 一种不对称化合物（Ⅳ）的制造方法，其特征在于，在不对称脲化合物（I）的存在下，使化合物（II）通过共轭加成而添加亲核试剂（III）。 还提供能够实现高收率且高度立体选择性的非对称共轭加成反应的非金属不对称催化剂。 该方法是通过其中使用催化剂的不对称共轭加成反应制备不对称化合物的有利方法。 [式中，X表示氧或硫; C *，C **和C ***各自表示不对称碳; R 1，R 2，R 4，R 5，R 8，R 9和R 10各自表示任选取代的低级烷基等，条件是例如 R 4和R 5可以彼此键合以形成任选取代的杂环等; R 3表示任选取代的芳基等; R 6和R 7各自表示氢等; Nu表示-CR 16（COR 17）（COR 18）（其中R 16，R 17和R 18各自表示任选取代的低级烷基等）等; EWG表示吸电子基团。]

    ASYMMETRIC UREA COMPOUND AND PROCESS FOR PRODUING ASYMMETRIC COMPOUND BY ASYMMETRIC CONJUGATE ADDITION REACTION WITH THE SAME AS CATALYST
    94.
    发明申请
    ASYMMETRIC UREA COMPOUND AND PROCESS FOR PRODUING ASYMMETRIC COMPOUND BY ASYMMETRIC CONJUGATE ADDITION REACTION WITH THE SAME AS CATALYST 审中-公开
    不对称尿素化合物和不对称化合物的方法，通过不相容的添加反应与相同的催化剂

    公开(公告)号：WO2005000803A3

    公开(公告)日：2005-03-03

    申请号：PCT/JP2004009350

    申请日：2004-06-25

    Applicant: SUMITOMO CHEMICAL CO ,  TAKEMOTO YOSHIJI

    Inventor： TAKEMOTO YOSHIJI

    IPC: C07C201/12 ,  C07C205/51 ,  C07C205/53 ,  C07C205/55 ,  C07C231/10 ,  C07C235/78 ,  C07C269/06 ,  C07C271/22 ,  C07C275/30 ,  C07C335/16 ,  C07C335/18 ,  C07D20060101 ,  C07D209/08 ,  C07D209/56

    CPC classification number: C07C335/16 ,  C07B2200/07 ,  C07C205/51 ,  C07C205/53 ,  C07C205/55 ,  C07C269/06 ,  C07C275/30 ,  C07C335/18 ,  C07C2601/14 ,  C07C2602/10 ,  C07D209/08 ,  C07C271/22

    Abstract: A process for producing an asymmetric compound (IV), characterized by causing a compound (II) to add a nucleophilic reagent (III) through conjugate addition in the presence of an asymmetric urea compound (I). Also provided is a nonmetallic asymmetric catalyst capable of realizing asymmetric conjugate addition reaction which attain high yield and are highly stereoselective. The process is an advantageous process for producing an asymmetric compound by an asymmetric conjugate addition reaction in which the catalyst is used. [In the formulae, X represents oxygen or sulfur; C*, C**, and C*** each indicates asymmetric carbon; R , R , R , R , R , R , and R each represents optionally substituted lower alkyl, etc., provided that, for example, R and R may be bonded to each other to form an optionally substituted homocycle, etc.; R represents optionally substituted aryl, etc.; R and R each represents hydrogen, etc.; Nu represents -CR (COR )(COR ) (wherein R , R , and R each represents optionally substituted lower alkyl, etc.), etc.; and EWG represents an electron-withdrawing group.]

    Abstract translation: 一种不对称化合物（Ⅳ）的制造方法，其特征在于，在不对称脲化合物（I）的存在下，使化合物（II）通过共轭加成而添加亲核试剂（III）。 还提供能够实现高收率且高度立体选择性的非对称共轭加成反应的非金属不对称催化剂。 该方法是通过其中使用催化剂的不对称共轭加成反应制备不对称化合物的有利方法。 [式中，X表示氧或硫; C *，C **和C ***各自表示不对称碳; R 1，R 2，R 4，R 5，R 8，R 9和R 10各自表示任选取代的低级烷基等，条件是例如 R 4和R 5可以彼此键合以形成任选取代的杂环等; R 3表示任选取代的芳基等; R 6和R 7各自表示氢等; Nu表示-CR 16（COR 17）（COR 18）（其中R 16，R 17和R 18各自表示任意取代的低级烷基等）等; EWG表示吸电子基团。]

    AMINO ACID-N-CARBOXY ANHYDRIDES HVAING SUBSTITUENT AT NITROGEN
    96.
    发明申请
    AMINO ACID-N-CARBOXY ANHYDRIDES HVAING SUBSTITUENT AT NITROGEN 审中-公开
    氨基酸 - N-羧酸类异氰酸酯在氮中起作用

    公开(公告)号：WO02002538A1

    公开(公告)日：2002-01-10

    申请号：PCT/JP2001/005780

    申请日：2001-07-04

    IPC: C07C231/10 ,  C07C237/22 ,  C07D263/44 ,  C07D295/185 ,  C07D413/06 ,  C07D413/14 ,  C07D417/06 ,  C07D417/14 ,  C07D471/04 ,  C07D487/08 ,  C07D521/00 ,  C07D471/08

    CPC classification number: C07D263/44 ,  C07C231/10 ,  C07C237/22 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D295/185 ,  C07D413/06 ,  C07D413/14 ,  C07D417/06 ,  C07D417/14 ,  C07D471/04 ,  C07D487/08

    Abstract: Amino acid-N-carboxy anhydrides having an N-acyl substituent at nitrogen which are represented by the following general formula (1); and a process for producing the same. These compounds easily react with free amino acids, alcohols or nucleophilic agents such as anions and serve as useful intermediates in producing amino acid derivatives, optically active compounds, peptides, polypeptides and the like, which are useful in various fields including medicines and pesticides, at a high yield. Moreover, a process for producing diamides by using the compounds of the formula (1) with amine derivatives represented by the following general formula (7). These diamides are also appropriately usable in producing amino acid derivatives, optically active compounds, peptides, polypeptides and the like.

    Abstract translation: 在下列通式（1）表示的在氮气下具有N-酰基取代基的氨基酸-N-羧酸酐; 及其制造方法。 这些化合物容易与游离氨基酸，醇或亲核试剂如阴离子反应，并且可用作制备氨基酸衍生物，光学活性化合物，肽，多肽等的有用中间体，其可用于包括药物和农药在内的各种领域 高产量。 此外，通过使用式（1）的化合物与由以下通式（7）表示的胺衍生物制备二酰胺的方法。 这些二酰胺也可适用于制备氨基酸衍生物，光学活性化合物，肽，多肽等。

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