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    Novel arylpropyl aldehyde derivatives, processes for producing the same, and methods of using the same
    62.
    发明申请
    Novel arylpropyl aldehyde derivatives, processes for producing the same, and methods of using the same 失效
    新型芳基丙醛衍生物，其制备方法及其使用方法

    公开(公告)号：US20030032842A1

    公开(公告)日：2003-02-13

    申请号：US10197808

    申请日：2002-07-19

    Applicant: Ajinomoto Co., Inc.

    Inventor： Kenichi Mori ,  Shigeru Kawahara ,  Tadashi Takemoto

    IPC: C07C045/41 ,  C07C065/01

    CPC classification number: C07C69/734 ,  C07C45/41 ,  C07C47/27 ,  C07C47/277 ,  C07C51/367 ,  C07C59/64 ,  C07C59/52

    Abstract: 3-(3-Methyl-4-hydroxyphenyl)-3-methylbutyl aldehyde may be produced from 3-(3-methyl-4-hydroxyphenyl)-3-methylbutyric acid by converting the carboxyl group into a formyl group. N-nullN-null3-(3-methyl-4-hydroxyphenyl)-3-methylbutylnull-L-null-aspartylnull-L-phenylalanine 1-methyl ester, which is useful as a sweetener having a high potency of sweetness, can be easily and efficiently prepared on an industrial production from such an aldehyde derivative, via a reductive alkylation reaction with aspartame. Therefore, 3-(3-Methyl-4-hydroxyphenyl)-3-methylbutyl aldehyde is extremely excellent as an intermediate for the production of N-nullN-null3-(3-methyl-4-hydroxyphenyl)-3- methylbutylnull-L-null-aspartylnull-L-phenylalanine 1-methyl ester. The above butyric acid derivative is a novel compound, which can be easily produced by subjecting 3-(3-methyl-4-methoxyphenyl)-3-methylbutyric acid obtained by the reaction of 2-methoxytoluene with 3-methylcrotonic acid, to a reaction for converting a methoxy group into a hydroxyl group. The present invention further provides several novel compounds useful as a production intermediate, such as the above aldehyde derivative and the like.

    Abstract translation: 3-（3-甲基-4-羟基苯基）-3-甲基丁醛可以通过将羧基转变为甲酰基而由3-（3-甲基-4-羟基苯基）-3-甲基丁酸制备。 N- [N- [3-（3-甲基-4-羟基苯基）-3-甲基丁基] -L-α-天冬氨酰基] -L-苯丙氨酸1-甲基酯，其可用作具有高效能甜度的甜味剂 可以通过这种醛衍生物通过与阿斯巴甜的还原烷基化反应在工业生产上容易且有效地制备。 因此，3-（3-甲基-4-羟基苯基）-3-甲基丁基醛作为制备N- [N- [3-（3-甲基-4-羟基苯基）-3-甲基丁基] -L-α-天冬氨酰基] -L-苯丙氨酸1-甲酯。 上述丁酸衍生物是通过使2-甲氧基甲苯与3-甲基巴豆酸反应得到的3-（3-甲基-4-甲氧基苯基）-3-甲基丁酸与3-甲基巴豆酸反应，可以容易地制备的新化合物 用于将甲氧基转化为羟基。 本发明还提供了可用作生产中间体的几种新型化合物，例如上述醛衍生物等。

    Process for the preparation of a carboxylic acid
    66.
    发明授权
    Process for the preparation of a carboxylic acid 失效
    制备羧酸的方法

    公开(公告)号：US06444844B1

    公开(公告)日：2002-09-03

    申请号：US09817810

    申请日：2001-03-20

    Applicant: Abdul Majeed Seayad ,  Jayasree Seayad ,  Raghunath Vitthal Chaudhari

    Inventor： Abdul Majeed Seayad ,  Jayasree Seayad ,  Raghunath Vitthal Chaudhari

    IPC: C07C5110

    CPC classification number: C07C51/14 ,  C07C51/10 ,  C07C51/12 ,  C07C57/30 ,  C07C59/64 ,  C07C53/126

    Abstract: The present invention relates to a process for the preparation of a carboxylic acid of the formula III, wherein R1 is aryl, substituted aryl, naphthyl, substituted naphthyl or alkyl, R2, R3, R4 and R5 are independently hydrogen or alkyl, by reacting the corresponding olefin of formula I or the corresponding organic halide or alcohol of the formula II, wherein R1 is selected from the group consisting of aryl, substituted aryl, naphthyl, substituted naphthyl or alkyl, R2, R3, R4 and R5 are independently hydrogen or alkyl and X is a halogen atom or a —OH group, using a novel water soluble palladium complex catalyst of general formula IV wherein R1, R2 and R3 are substituents on the phosphine ligand and selected from the group consisting of alkyl, aryl, arylalkyl, and cycloaliphatic, at least one of which carries a sulfonic acid and salts thereof, X is aryl or alkyl sulfonato or aryl or alkyl carboxylate or formato or a halide, is an anionic chelating ligand containing a N donor and O— group.

    Abstract translation: 本发明涉及一种制备式Ⅲ羧酸的方法，其中R1是芳基，取代的芳基，萘基，取代的萘基或烷基，R2，R3，R4和R5独立地是氢或烷基， 式I的相应的烯烃或式II的相应的有机卤化物或醇，其中R 1选自芳基，取代的芳基，萘基，取代的萘基或烷基，R 2，R 3，R 4和R 5独立地是氢或烷基 并且X是卤素原子或-OH基团，使用新的通式IV的水溶性钯络合物催化剂，其中R 1，R 2和R 3是膦配体上的取代基，并且选自烷基，芳基，芳基烷基和环脂族 ，其中至少一个携带磺酸及其盐，X是芳基或烷基磺酸根或芳基或烷基羧酸酯或格式或卤素，是含有N供体和O-基团的阴离子螯合配体。

    Biphenyl-5-alkanoic acid derivatives and use thereof
    67.
    发明授权
    Biphenyl-5-alkanoic acid derivatives and use thereof 失效
    联苯基-5-链烷酸衍生物及其用途

    公开(公告)号：US06376546B1

    公开(公告)日：2002-04-23

    申请号：US09509683

    申请日：2000-06-08

    Applicant: Motoshi Shoda ,  Hiromichi Itoh

    Inventor： Motoshi Shoda ,  Hiromichi Itoh

    IPC: A61K3119

    CPC classification number: C07C235/16 ,  C07C59/64 ,  C07C59/72 ,  C07C59/90 ,  C07C205/56 ,  C07C233/54 ,  C07C235/20 ,  C07C235/34 ,  C07C275/42 ,  C07C307/10 ,  C07C311/08 ,  C07C2601/08 ,  C07C2601/14

    Abstract: Compounds represented by general formula I or salts thereof, wherein n is an integer of 2 or 3; R represents a straight-chain or branched saturated alkyl group having 4 or 4 carbon atoms, a cyclopentyl group, a cyclohexyl group or the like, Y represents a hydroxyl or amino group, A represents a hydrogen atom, a hydroxyl, methoxy, nitro group or the like, Q represents a hydrogen atom or a hydroxyl or methoxy group. They can be formulated to give pharmaceutical compositions that are effective as prophylactic or therapeutic agents for allergic diseases associated with IgE production inhibitors or IgE antibodies.

    Abstract translation: 由通式I表示的化合物或其盐，其中n为2或3的整数; R表示具有4或4个碳原子的直链或支链饱和烷基，环戊基，环己基等，Y表示羟基或氨基，A表示氢原子，羟基，甲氧基，硝基 Q表示氢原子或羟基或甲氧基。 它们可以配制成具有作为与IgE产生抑制剂或IgE抗体相关的过敏性疾病的预防或治疗剂有效的药物组合物。

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