利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

228 条记录 (耗时 0.019 秒)

    4-PYRROLIDINO-PHENYL-BENZYL ETHER DERIVATIVES
    23.
    发明申请
    4-PYRROLIDINO-PHENYL-BENZYL ETHER DERIVATIVES 审中-公开
    4-吡咯烷基 - 苯基 - 苯甲醚衍生物

    公开(公告)号：WO2004026826A1

    公开(公告)日：2004-04-01

    申请号：PCT/EP2003/010383

    申请日：2003-09-18

    申请人： F. HOFFMANN-LA ROCHE AG

    发明人： JOLIDON, Synese ,  RODRIGUEZ-SARMIENTO, Rosa, Maria ,  THOMAS, Andrew, William ,  WOSTL, Wolfgang ,  WYLER, Rene

    IPC分类号： C07D207/26

    CPC分类号： C07D207/273 ,  C07D207/277

    摘要： Racemic or enantiomerically pure 4-pyrrolidino derivatives of formula (I), processes for their preparation, pharmaceutical compositions comprising said derivatives, and their use in the prevention and treatment of illness, e.g. which are mediated by monoamine oxidase B inhibitors, in particular Alzheimer's disease or senile dementia.

    摘要翻译： 式（I）的外消旋或对映异构体纯的4-吡咯烷子基衍生物，其制备方法，包含所述衍生物的药物组合物及其在预防和治疗疾病中的用途。 其由单胺氧化酶B抑制剂介导，特别是阿尔茨海默病或老年痴呆。

    PROCESS FOR THE ENANTIOSELECTIVE SYNTHESIS OF HYDROXYPYRROLIDINES FROM AMINO ACIDS AND PRODUCTS THEREOF
    30.
    发明申请
    PROCESS FOR THE ENANTIOSELECTIVE SYNTHESIS OF HYDROXYPYRROLIDINES FROM AMINO ACIDS AND PRODUCTS THEREOF 审中-公开
    氨基酸及其制品的羟基吡咯烷酮的选择性合成方法

    公开(公告)号：WO99046243A1

    公开(公告)日：1999-09-16

    申请号：PCT/US1998/000941

    申请日：1998-03-12

    IPC分类号： C07D207/12 ,  C07D207/26 ,  C07D207/273 ,  C07D263/10 ,  C07D263/14 ,  C07D277/14

    CPC分类号： C07D207/273 ,  C07D207/12 ,  C07D263/10

    摘要： The present invention relates to processes for the enantioselective synthesis of hydroxypyrrolidines from amino acids. An amino methyl ester is used as the starting material. The ester is reacted with a benziminoethyl ether to produce an oxazoline or thiazoline. Specifically, L-serine methyl ester is used to produce 4-(carbomethoxy)-2-phenyl- DELTA -oxazoline, and cysteine is used to produce the corresponding thiazoline. The oxazoline (or thiazoline) can be reduced to an aldehyde by treatment with a slight excess of DIBAL-H. The oxazoline is quenched with alcohol and reacted with (carbomethoxymethylene) triphenylphosphorane, to produce (S)-(+)-methyl (E)- and (S)-(-)-methyl (Z)-3-(4,5-dihydro-2-phenyl-4-oxazolyl)-2-propenoate. The double bond is hydroxylated to yield the diol esters. The resulting diol is then treated with aqueous acid to hydrolyze the oxazoline and recyclize to produce 3,4-dihydroxy-5-hydroxymethylpyrrolidone benzoate. This is treated with an excess of borane in tetrahydrofuran to yield (2-hydroxymethyl) 3,4-dihydroxypyrrolidine. The intermediate compounds are useful both in the present process and as final products themselves. The total yield of the mixture of isomers, as well as their ratio, can be varied.

    摘要翻译： 本发明涉及从氨基酸对映选择性合成羟基吡咯烷的方法。 使用氨基甲酯作为原料。 酯与苯甲亚乙基醚反应生成恶唑啉或噻唑啉。 具体地说，使用L-丝氨酸甲酯来制备4-（甲酯基）-2-苯基-TATA 2 - 恶唑啉，半胱氨酸用于制备相应的噻唑啉。 恶唑啉（或噻唑啉）可以通过用稍微过量的DIBAL-H处理而还原成醛。 恶唑啉用醇淬灭并与（甲酯基亚甲基）三苯基正膦反应生成（S） - （+） - 甲基（E） - 和（S） - （ - ） - 甲基（Z）-3- 二氢-2-苯基-4-恶唑基）-2-丙烯酸乙酯。 羟基化双键得到二醇酯。 然后将所得二醇用酸水溶液处理以水解恶唑啉并再循环以产生3,4-二羟基-5-羟甲基吡咯烷酮苯甲酸酯。 在四氢呋喃中用过量的硼烷处理，得到（2-羟甲基）3,4-二羟基吡咯烷。 中间体化合物在本方法中可用作最终产物本身。 异构体混合物的总产率及其比例可以变化。