Process for the synthesis of benzothiadiazole compounds
    12.
    发明授权
    Process for the synthesis of benzothiadiazole compounds 有权
    合成苯并噻二唑化合物的方法

    公开(公告)号:US09440965B2

    公开(公告)日:2016-09-13

    申请号:US13809646

    申请日:2011-07-13

    IPC分类号: C07D285/14 C07D417/14

    CPC分类号: C07D417/14 C07D285/14

    摘要: The invention relates to a significantly improved process for the preparation of benzothiadxazole compounds which can be used in the production of Luminescent Solar Concentrators, (LSC). In particular, the synthesis process of the present invention is oriented towards the preparation of 4,-di-2-thienyl-2,1,3-benzo-thiadiazole.

    摘要翻译: 本发明涉及可用于生产发光太阳能集中器(LSC)的苯并噻唑化合物的制备方法。 特别地,本发明的合成方法取决于制备4'-二-2-噻吩基-2,1,3-苯并噻二唑。

    Process for the preparation of stable nitroxyl radicals
    13.
    发明授权
    Process for the preparation of stable nitroxyl radicals 有权
    制备稳定硝酰自由基的方法

    公开(公告)号:US07982052B2

    公开(公告)日:2011-07-19

    申请号:US12161283

    申请日:2007-02-09

    IPC分类号: C07D209/44

    CPC分类号: C07D209/46

    摘要: Process for the preparation of stable nitroxyl radicals (I) starting from N-benzylphthalimide in two steps. In the first step, the intermediate N-benzyl-1,1,3,3-tetra-alkylisoindoline is prepared by treatment with a Grignard reagent, prepared in methyl-tert-butyl ether, of N-benzylphthalimide, obtained in the same reaction environment starting from phthalic anhydride and benzylamine. In the second step, the N-benzyl-1,1,3,3-tetra-alkylisoindoline is transformed into the nitroxyl radical by hydrogenolysis and subsequent oxidation with hydrogen peroxide in the presence of a catalyst selected from acids and salts of polymolybdic or polytungstic acids.

    摘要翻译: 从N-苄基邻苯二甲酰亚胺开始制备稳定的硝酰基(I)的方法分两步进行。 在第一步中,中间体N-苄基-1,1,3,3-四烷基异吲哚啉通过用在相同反应中获得的N-苄基邻苯二甲酰亚胺的甲基叔丁基醚中制备的格氏试剂进行处理 环境从邻苯二甲酸酐和苄胺开始。 在第二步中,N-苄基-1,1,3,3-四烷基异吲哚啉通过氢解反应转化为硝酰基,随后在选自酸和多钼或多元酸的盐的催化剂存在下用过氧化氢氧化 酸。

    Perfected process for the preparation of stable nitroxide radicals
    17.
    发明授权
    Perfected process for the preparation of stable nitroxide radicals 有权
    用于制备稳定的氮氧自由基的完美工艺

    公开(公告)号:US07745478B2

    公开(公告)日:2010-06-29

    申请号:US11574582

    申请日:2005-08-25

    IPC分类号: A61K31/404

    CPC分类号: C07D209/44

    摘要: Process for the preparation of stable nitroxide radicals (I) starting from N-benzylphthalimide in three steps. In the first step, the N-benzylphthalimide is transformed into N-benzyl-1,1,3,3-tetralkylisoindoline by treatment with a Grignard reagent prepared in methyl-tert-butyl ether. In the second step, the N-benzyl-1,1,3,3-tetraalkylisoindoline is transformed into 1,1,3,3-tetra-alkylisoindoline by hydrogenolysis. In the third step, the 1,1,3,3-tetra-alkyl-isoindoline is transformed into the nitroxide radical by oxidation with hydrogen peroxide in the presence of a catalyst selected from acids and salts of polymolybdic or polytungstic acids.

    摘要翻译: 从N-苄基邻苯二甲酰亚胺开始三步制备稳定的氮氧自由基(I)的方法。 在第一步中,通过用在甲基叔丁基醚中制备的格氏试剂处理,将N-苄基邻苯二甲酰亚胺转化成N-苄基-1,1,3,3-四烷基异吲哚啉。 在第二步中,N-苄基-1,1,3,3-四烷基异吲哚啉通过氢解转化为1,1,3,3-四烷基异吲哚啉。 在第三步中,通过在选自酸和多钼酸或多钨酸的盐的催化剂的存在下,用过氧化氢氧化将1,1,3,3-四烷基 - 异吲哚啉转化为硝基氧基。

    Process for preparing L(-)-carnitine chloride
    19.
    发明授权
    Process for preparing L(-)-carnitine chloride 失效
    制备L( - ) - 肉碱氯化物的方法

    公开(公告)号:US5248601A

    公开(公告)日:1993-09-28

    申请号:US595670

    申请日:1990-10-09

    IPC分类号: C12P17/02 C12P41/00

    CPC分类号: C12P17/02 C12P41/005

    摘要: A biotechnological process for preparing L(-)-carnitine chloride, having the formula ##STR1## comprising: (a) reacting a racemic ester of (R,S)-3,4-epoxybutyric acid having the formula ##STR2## wherein R is an alkyl group having from 1 to 10 carbons or a benzyl group, with an enzyme capable of selectively hydrolyzing enantiomer S(-);(b) separating the enantiomer S(-) from non-reacted ester which is present in predominantly the R(+) form;(c) reacting the non-reacted ester obtained in step (b) with an enzyme capable of quantitatively hydrolyzing the R(+) form to obtain thereby a salt of 3,4-epoxybutyric acid in the R(+) form having the formula ##STR3## wherein X is Na, K, or Li; (d) reacting the salt obtained in step (c) with a molar excess of trimethylamine; and(e) treating the reaction product of step (d) with HCl to remove excess trimethylamine and to obtain thereby the L(-)-carnitine chloride of formula (I).

    摘要翻译: 用于制备具有式(I)的L( - ) - 肉碱氯化物的生物技术方法包括:(a)使具有式(IMA)的(R,S)-3,4-环氧丁酸的外消旋酯与式 (II)其中R为具有1至10个碳原子的烷基或苄基,具有能够选择性水解对映体S( - )的酶; (b)从主要为R(+)形式存在的未反应的酯分离对映体S( - ); (c)将步骤(b)中获得的未反应的酯与能够定量水解R(+)形式的酶反应,从而得到具有式(B)的R(+)形式的3,4-(环己基) (III)其中X是Na,K或Li; (d)使步骤(c)中获得的盐与摩尔过量的三甲胺反应; 和(e)用HCl处理步骤(d)的反应产物以除去过量的三甲胺,从而得到式(I)的L( - ) - 肉碱氯化物。

    Process for preparing L(-)-carnitine chloride from 3,4-epoxybutyric
esters and novel intermediate compounds
    20.
    发明授权
    Process for preparing L(-)-carnitine chloride from 3,4-epoxybutyric esters and novel intermediate compounds 失效
    从3,4-环氧丁酸酯和新型中间体化合物制备L( - ) - 肉碱氯化物的方法

    公开(公告)号:US4865771A

    公开(公告)日:1989-09-12

    申请号:US25351

    申请日:1987-03-13

    CPC分类号: C12P41/005 C12P17/02

    摘要: A process for preparing L(-)-carnitine chloride having the formula: ##STR1## comprising the steps of: (a) reacting a racemic ester of (R,S)-3,4-epoxybutyric acid having the formula: ##STR2## wherein R is an alkyl group having from 1-10 carbons, or a benzyl group, with an enzyme capable of selectively hydrolyzing enantiomer S(-),(b) separating said enantiomer S(-), from non-reacted ester, which is predominantly in the R(+) form;(c) reacting (1) the non-reacted ester obtained in step (b) with trimethylamine hydrochlorid or (2) the trimethylamine, to obtain thereby an ester having the formula: ##STR3## (d) hydrolyzing the ester obtain in step (c) in the presence of HCl to obtain thereby the L(-)-carnitine chloride having formula (I).The present invention is also directed to a novel class of compounds comprising R(+) enantiomers of the esters of 3,4-epoxybutyric acid.

    摘要翻译: 一种具有下式的制备L( - ) - 肉碱氯化物的方法:(I)包括以下步骤:(a)使具有下式的(R,S)-3,4-环氧丁酸的外消旋酯: (II)其中R是具有1-10个碳原子的烷基或苄基,具有能够选择性水解对映异构体S( - )的酶,(b)将所述对映异构体S( - )与非 - 主要是R(+)形式的酯; (c)使(1)步骤(b)中获得的未反应的酯与三甲胺盐酸盐或(2)三甲胺反应,从而得到具有下式的酯:(Ⅳ)(d)水解该酯 在步骤(c)中,在HCl存在下得到具有式(I)的L( - ) - 肉碱氯化物。 本发明还涉及包含3,4-环氧丁酸的酯的R(+)对映异构体的新一类化合物。