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18 条记录 (耗时 0.037 秒)

    Arylalkanoic acid process improvement
    1.
    发明授权
    Arylalkanoic acid process improvement 失效
    芳烷基酸工艺改进

    公开(公告)号：US4623736A

    公开(公告)日：1986-11-18

    申请号：US396967

    申请日：1982-07-09

    申请人： Jerry A. Walker ,  Sanjay I. Amin

    发明人： Jerry A. Walker ,  Sanjay I. Amin

    IPC分类号： C07C67/00 ,  B01J31/00 ,  B01J31/04 ,  C07B61/00 ,  C07C45/46 ,  C07C49/80 ,  C07C49/813 ,  C07C49/84 ,  C07C51/02 ,  C07C51/09 ,  C07C69/612 ,  C07C69/65 ,  C07D319/08 ,  C07D319/06 ,  C07C69/76

    CPC分类号： C07D319/08 ,  C07C45/46 ,  C07C49/80 ,  C07C49/813 ,  C07C49/84 ,  C07C51/02 ,  C07C51/09

    摘要： In preparing arylalkanoic acids, e.g. ibuprofen or naproxen, via the conversion of the selected .alpha.-haloketal derivative of a 1-haloethyl aryl ketone to the haloalkyl ester of the arylalkanoic acid using a zinc salt catalyst the improvement comprising reacting a ring-substituted 6-membered ring ketal of the selected 1-haloethyl C.sub.6 -C.sub.12 -aryl ketone with a soluble zinc carboxylate salt to form the corresponding 3-haloalkyl arylalkanoic acid ester. The ester is converted to the alkali metal salt of the acid with base in an aqueous/water insoluble organic liquid mixture and the crude salt is converted to the corresponding acid in an aqueous/water insoluble solvent mixture for the acid, the organic solution of the acid is washed with a pH 7.0 to 8.0 buffer solution, and the arylalkanoic acid product is separated from the mother liquor which mother liquor is recycled to the alkali metal arylalkanoate salt forming step of the process to accumulate and recover the arylalkanoic acid values which remained in the mother liquor.

    摘要翻译： 在制备芳基链烷酸时，例如 布洛芬或萘普生，通过使用锌盐催化剂将1-卤代乙基芳基酮的所选α-卤代酮衍生物转化为芳基链烷酸的卤代烷基酯，其改进包括使所选择的环取代的6-元环缩酮反应 1-卤代乙基C6-C12-芳基酮与可溶性羧酸锌盐形成相应的3-卤代烷基芳基链烷酸酯。 该酯在水/水不溶性有机液体混合物中用碱转化为酸的碱金属盐，并将粗盐转化为酸/水不溶性溶剂混合物中相应的酸，酸的有机溶液 用pH7.0至8.0的缓冲溶液洗涤酸，并将芳基链烷酸产物与母液中的母液分离，将母液循环至形成碱金属芳基烷酸盐的步骤，以积累并回收残留在芳基链烷酸中的芳基链烷酸值 母酒。

    Processes for the preparation of hydratropic acids and esters
    4.
    发明授权
    Processes for the preparation of hydratropic acids and esters 失效
    制备水合酸和酯的方法

    公开(公告)号：US4324904A

    公开(公告)日：1982-04-13

    申请号：US105166

    申请日：1979-12-19

    申请人： Thomas A. Hylton ,  Jerry A. Walker

    发明人： Thomas A. Hylton ,  Jerry A. Walker

    IPC分类号： C07C51/38 ,  C07C205/56 ,  C07C69/76

    CPC分类号： C07C205/56 ,  C07C51/38

    摘要： The invention concerns the novel compounds dialkyl 2-(3-fluoro-4-nitrophenyl)-2-methylmalonate IIIa and dialkyl 2-(3-fluoro-4-aminophenyl)-2-methylmalonate IVa useful as intermediates in an improved process for making 2-(2-fluoro-4-biphenylyl)propionic acid, known as flurbiprofen, having the formula ##STR1## and ester thereof. It has anti-inflammatory activity which is about 240 times that of aspirin and analgesic activity which is about 180 times that of aspirin in standard laboratory tests. However, despite this high activity, the toxicity (LD.sub.50) is only 1.2 to 2.4 times greater than that of aspirin in standard laboratory tests.Also within the invention is a novel method of making the above intermediates and analogs thereof useful to prepare corresponding biaryl compounds which have pharmaceutical uses.

    摘要翻译： 本发明涉及新型化合物2-（3-氟-4-硝基苯基）-2-甲基丙二酸二烷基酯IIIa和2-（3-氟-4-氨基苯基）-2-甲基丙二酸二烷基酯IVa，其用作改进的制备方法中的中间体 称为氟比洛芬的2-（2-氟-4-联苯基）丙酸，其具有式Ia及其酯。 它具有约240倍的阿斯匹林和止痛活性的抗炎活性，约为阿司匹林在标准实验室检测中的约180倍。 然而，尽管活性高，但在标准实验室检测中，毒性（LD50）仅为阿司匹林的1.2〜2.4倍。 本发明还有一种使上述中间体及其类似物用于制备具有药物用途的相应联芳基化合物的新方法。

    Process for preparing arylalkanoic acid derivatives
    5.
    发明授权
    Process for preparing arylalkanoic acid derivatives 失效
    制备芳基酸衍生物的方法

    公开(公告)号：US4135051A

    公开(公告)日：1979-01-16

    申请号：US807032

    申请日：1977-06-16

    申请人： Jerry A. Walker

    发明人： Jerry A. Walker

    IPC分类号： C07C41/56 ,  C07C43/166 ,  C07C43/303 ,  C07C45/46 ,  C07C49/76 ,  C07C49/82 ,  C07C51/09 ,  C07C67/00 ,  C07C69/76

    CPC分类号： C07C45/46 ,  C07C41/28 ,  C07C41/56 ,  C07C49/76 ,  C07C49/82 ,  C07C51/09

    摘要： 2-Aryl-C.sub.3 to C.sub.6 -alkanoate esters are prepared economically by reacting an enol ether of an aryl alkyl ketone with a trivalent thallium salt in an organic solvent. The trivalent thallium ions can be regenerated by adding a peracid and a reactive form of manganese, ruthenium, cobalt, iridium, hafnium, osmium or neobium to oxidize monovalent thallium ions to the trivalent state, in a sequential, continuous or stoichiometric procedure. The ester intermediate product is then converted to the corresponding 2-aryl-C.sub.3 - to C.sub.6 -alkanoic acid or salt thereof. The aryl group is selected so the resulting acid product will be a useful compound such as anti-inflammatory, analgesic and anti-pyretic drug or agriculturally useful product. Examples of drug acids which can be made by this process include ibuprofen, flurbiprofen, fenoprofen and naproxen and the like.

    Malonic acids and esters thereof
    10.
    发明授权
    Malonic acids and esters thereof 失效
    丙二酸及其酯

    公开(公告)号：US4398035A

    公开(公告)日：1983-08-09

    申请号：US193660

    申请日：1980-10-03

    申请人： Jerry A. Walker

    发明人： Jerry A. Walker

    IPC分类号： C07C57/58 ,  C07C55/08 ,  C07C69/38

    CPC分类号： C07C57/58

    摘要： The invention concerns the novel compounds dialkyl 2-(3-fluoro-4-nitrophenyl)-2-methylmalonate IIIa and dialkyl 2-(3-fluoro-4-aminophenyl)-2-methylmalonate IVa useful as intermediates in an improved process for making 2-(2-fluoro-4-biphenylyl)propionic acid, known as flurbiprofen, having the formula ##STR1## and ester thereof. It has anti-inflammatory activity which is about 240 times that of aspirin and analgesic activity which is about 180 times that of aspirin in standard laboratory tests. However, despite this high activity, the toxicity (LD.sub.50) is only 1.2 to 2.4 times greater than that of aspirin in standard laboratory tests.Also within the invention is a novel method of making the above intermediates and analogs thereof useful to prepare corresponding biaryl compounds which have pharmaceutical uses.

    摘要翻译： 本发明涉及新型化合物2-（3-氟-4-硝基苯基）-2-甲基丙二酸二烷基酯IIIa和2-（3-氟-4-氨基苯基）-2-甲基丙二酸二烷基酯IVa，其用作改进的制备方法中的中间体 称为氟比洛芬的2-（2-氟-4-联苯基）丙酸，其具有式Ia及其酯。 它具有约240倍的阿斯匹林和止痛活性的抗炎活性，约为阿司匹林在标准实验室检测中的约180倍。 然而，尽管活性高，但在标准实验室检测中，毒性（LD50）仅为阿司匹林的1.2〜2.4倍。 本发明还有一种使上述中间体及其类似物用于制备具有药物用途的相应联芳基化合物的新方法。