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    N-acylamino acid derivatives
    5.
    发明授权
    N-acylamino acid derivatives 失效
    N-酰基氨基酸衍生物

    公开(公告)号：US5319082A

    公开(公告)日：1994-06-07

    申请号：US868140

    申请日：1992-04-14

    Applicant: Hajime Morishima ,  Yutaka Koike ,  Masato Nakano ,  Shugo Atsuumi ,  Seiichi Tanaka ,  Kenji Matsuyama

    Inventor： Hajime Morishima ,  Yutaka Koike ,  Masato Nakano ,  Shugo Atsuumi ,  Seiichi Tanaka ,  Kenji Matsuyama

    IPC: A61K31/195 ,  A61K31/535 ,  C07C59/66 ,  C07C317/00 ,  C07C317/44 ,  C07C323/43 ,  C07D207/08 ,  C07D211/14 ,  C07D215/12 ,  C07D233/54 ,  C07D239/38 ,  C07D257/04 ,  C07D265/30 ,  C07D285/12 ,  C07D285/125 ,  C07D295/084 ,  C07D295/12 ,  C07D295/125 ,  C07D295/13 ,  C07D295/24 ,  C07D307/38 ,  C07D319/18 ,  C07D401/12 ,  C07F7/18 ,  C07D413/12

    CPC classification number: C07D207/08 ,  C07C323/00 ,  C07C323/43 ,  C07C59/66 ,  C07D211/14 ,  C07D215/12 ,  C07D233/64 ,  C07D239/38 ,  C07D257/04 ,  C07D285/125 ,  C07D295/084 ,  C07D295/125 ,  C07D295/13 ,  C07D295/24 ,  C07D307/38 ,  C07D319/18 ,  C07D401/12 ,  C07F7/1856

    Abstract: An N-acylamino acid derivative of the formula: ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.4 and R.sup.6 is hydrogen, lower alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl or a monocyclic or bicyclic heterocyclic group containing from 1 to 4 hetero atoms; each of R.sup.3 and R.sup.5 is hydrogen or lower alkyl; A is --CH(OH)--(CH.sub.2).sub.q R.sup.7 wherein R.sup.7 is hydrogen, lower alkyl, cycloalkyl, cyloalkylalkyl, aryl, aralkyl, a-monocyclic or bicyclic heterocyclic group containing from 1 to 4 hetero atoms or --E--R.sup.10 wherein E is --S(O).sub.i -- wherein i is 0, 1 or 2, oxygen, --NR.sup.11 -- wherein R.sup.11 is hydrogen, lower alkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl, or ##STR2## wherein each of R.sup.12 and R.sup.13 is hydrogen, lower alkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl, and R.sup.10 is hydrogen, lower alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl or a monocyclic or bicyclic heterocyclic group containing from 1 to 4 hetero atoms provided that when R.sup.10 is hydrogen, i is 0, and a is an integer of from 0 to 5; or --CH.sub.2 --CHR.sup.8 --CO--R.sup.9 wherein R.sup.8 is hydrogen, lower alkyl, cycloalkyl, cycloalkylakyl, aryl, aralkyl or a monocyclic or bicyclic heterocyclic group containing from 1 to 4 hetero atoms, and R.sup.9 is hydroxyl, --OX wherein, X is alkyl aryl, lower alkoxycarbonyloxyalkyl or 1-phthalidyl, or --N(Y.sup.1)(Y.sup.2 ) wherein each of Y.sup.1 and Y.sup.2 is hydrogen, lower alkyl, aryl, aralkyl or cycloalkyl, or Y.sup.1 and Y.sup.2 form together with the adjacent nitrogen atom a 5- or 6-membered heterocyclic group which may contain a further hetero from; m is 0, 1 or 2; and n is an integer of from 1 to 5, provided that when R.sup.1 is hydrogen, m is 0; or a salt thereof, which is useful as hypotensive drugs.

    Abstract translation: 下式的N-酰基氨基酸衍生物：其中R 1，R 2，R 4和R 6各自为氢，低级烷基，环烷基，环烷基烷基，芳基，芳烷基或单环或双环杂环基，其含有1至 4个杂原子; R 3和R 5各自为氢或低级烷基; A是-CH（OH） - （CH 2）q R 7，其中R 7是含有1至4个杂原子的氢，低级烷基，环烷基，环烷基烷基，芳基，芳烷基，α-单环或双环杂环基或-E-R 10，其中E是 -S（O）i - 其中i是0,1或2，氧，-NR 11 - ，其中R 11是氢，低级烷基，环烷基，环烷基烷基，芳基或芳烷基，或者其中R 12和R 13各自是氢， 低级烷基，环烷基，环烷基烷基，芳基或芳烷基，R 10为含有1至4个杂原子的氢，低级烷基，环烷基，环烷基烷基，芳基，芳烷基或单环或双环杂环基，条件是当R 10为氢时，i为0 a为0〜5的整数， 或-CH 2 -CHR 8 -CO-R 9，其中R 8是氢，低级烷基，环烷基，环烷基烷基，芳基，芳烷基或含有1至4个杂原子的单环或双环杂环基，并且R 9是羟基， 烷基芳基，低级烷氧基羰氧基烷基或1-邻苯二甲酰基，或-N（Y1）（Y2）其中Y 1和Y 2分别为氢，低级烷基，芳基，芳烷基或环烷基或Y1和Y2各自与相邻的氮原子一起形成5-或 可含有另外的杂原子的6元杂环基; m为0,1或2; 且n为1至5的整数，条件是当R 1为氢时，m为0; 或其盐，其可用作降压药物。

    Process for obtaining enantiomers of 2-arylpropionic acids
    9.
    发明授权
    Process for obtaining enantiomers of 2-arylpropionic acids 失效
    获得2-芳基丙酸对映​​异构体的方法

    公开(公告)号：US4973745A

    公开(公告)日：1990-11-27

    申请号：US345716

    申请日：1989-05-01

    Applicant: Gottfried Blaschke ,  Karl-Ernst Schulte

    Inventor： Gottfried Blaschke ,  Karl-Ernst Schulte

    IPC: C07B55/00 ,  C07B57/00 ,  C07C51/353 ,  C07C51/487 ,  C07C57/30 ,  C07C57/32 ,  C07C57/58 ,  C07C59/64 ,  C07C59/66 ,  C07D209/88

    CPC classification number: C07D209/88 ,  C07C51/487

    Abstract: A process for obtaining enantiomers of 2-arylpropionic acids by reacting a racemic mixture thereof with an amine-enantiomer, which process comprises converting the racemate of the 2-arylpropionic acid with an optically active form of threo-1-p-nitrophenyl-2-aminopropane-1,3-diol into the diastereomeric salts, separating these salts and converting the thus-obtained pure diastereomers into the free acids of the enantiomer forms of the 2-arylpropionic acid or into the salts thereof.

    Abstract translation: 通过使其外消旋混合物与胺对映体反应获得2-芳基丙酸的对映异构体的方法，该方法包括将2-芳基丙酸的外消旋物与旋光活性形式的苏氨-1-对硝基苯基-2- 氨基丙烷-1,3-二醇转化成非对映体盐，分离这些盐并将由此得到的纯非对映异构体转化为2-芳基丙酸的对映体形式的游离酸或其盐。

    Process for the production of carboxymethylated alchols, ether alcohols, thioalcohols, or alkyl phenols
    10.
    发明授权
    Process for the production of carboxymethylated alchols, ether alcohols, thioalcohols, or alkyl phenols 失效
    制备羧甲基化的醇，醚醇，硫代醇或烷基酚的方法

    公开(公告)号：US4625057A

    公开(公告)日：1986-11-25

    申请号：US522771

    申请日：1983-08-12

    Applicant: Hermann Springmann ,  Kurt Kosswig

    Inventor： Hermann Springmann ,  Kurt Kosswig

    IPC: C07C59/125 ,  C07C51/00 ,  C07C51/367 ,  C07C59/305 ,  C07C59/48 ,  C07C59/58 ,  C07C59/60 ,  C07C59/66 ,  C07C59/70 ,  C07C67/00 ,  C07C313/00 ,  C07C319/14 ,  C07C323/52

    CPC classification number: C07C51/367 ,  C07C319/12

    Abstract: A process for the production of carboxymethylates comprises reacting alcohols, ether alcohols, or alkyl phenols with an aqueous solution of at most a stoichiometric amount of free chloroacetic acid and twice the stoichiometric amount of an aqueous base. The chloroacetic acid and base are added separately, but simultaneously under agitation (at elevated temperature and under reduced pressure) to the alcohol or alkyl phenol. The water content in the reaction mixture, during the entire reaction, is maintained at 0.3-1.5% by weight. Increased selectivity results and it now becomes possible to use aqueous chloroacetic acid in this process.

    Abstract translation: 制备羧甲基化物的方法包括使醇，醚醇或烷基酚与至多化学计量的游离氯乙酸和两倍化学计量的碱水溶液的水溶液反应。 分别加入氯乙酸和碱，但同时在搅拌（在升高的温度和减压下）加入到醇或烷基苯酚中。 在整个反应期间，反应混合物中的水含量保持在0.3-1.5重量％。 增加的选择性结果，现在可以在该方法中使用氯乙酸水溶液。

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