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    Method for preparing phosphinic acids used in preparing ace inhibitors and intermediates produced thereby
    1.
    发明授权
    Method for preparing phosphinic acids used in preparing ace inhibitors and intermediates produced thereby 失效
    制备用于制备ace抑制剂的次膦酸的方法及其制备的中间体

    公开(公告)号：US4873356A

    公开(公告)日：1989-10-10

    申请号：US102694

    申请日：1987-09-30

    申请人： Edward W. Petrillo, Jr. ,  Donald S. Karanewsky ,  John K. Thottathil ,  James E. Heikes ,  John A. Grosso

    发明人： Edward W. Petrillo, Jr. ,  Donald S. Karanewsky ,  John K. Thottathil ,  James E. Heikes ,  John A. Grosso

    IPC分类号： A61K31/66 ,  A61P9/12 ,  A61P43/00 ,  B01J23/44 ,  C07B61/00 ,  C07F9/32 ,  C12N9/99

    CPC分类号： C07F9/3264 ,  C07F9/3211

    摘要： A method is provided for preparing phosphinic acid compounds, which are useful in preparing certain angiotensin converting enzyme inhibitors, which have the formula ##STR1## wherein R.sub.1 is lower alkyl, aryl, arylalkyl, cycloalkyl or cycloalkylalkyl;R.sub.2 is hydrogen, lower alkyl or arylalkyl;X is hydrogen, lower alkyl or phenyl;Y is hydrogen, lower alkyl, phenyl or alkoxy, or together X and Y are --(CH.sub.2).sub.2 --, --(CH.sub.2).sub.3 --, --CH.dbd.CH--, or ##STR2## and n is 0 or 1including salts thereof and stereoisomers thereof, which method includes the steps of reacting a phosphinic acid ester of the structure ##STR3## wherein R.sub.3 is a group removable by hydrogenolysis such as benzyl or substituted benzyl, with a halo ester of the structure ##STR4## in the presence of an organic base to form a phosphinic acid ester of the structure ##STR5## hydrogenating the above ester to form a diastereomic mixture of a phosphinic acid of the structure ##STR6## recrystallizing to recover the preferred racemic mixture and resolving same employing a resolving agent, preferably L-cinchonidine, to form the corresponding resolved salt which may be acidified to the corresponding acid. In addition, novel intermediates which are acids and salts as described above are also provided.

    摘要翻译： 提供了一种制备次膦酸化合物的方法，其可用于制备具有下式的其中R 1为低级烷基，芳基，芳烷基，环烷基或环烷基烷基的一些血管紧张素转换酶抑制剂; R2是氢，低级烷基或芳基烷基; X是氢，低级烷基或苯基; Y是氢，低级烷基，苯基或烷氧基，或者一起X和Y是 - （CH 2）2 - ， - （CH 2）3 - ， - CH = CH-或，n是0或1，包括其盐 该方法包括以下步骤：使结构式“其中R3是通过氢解可除去的基团如苄基或取代的苄基”的结构式的次膦酸酯与结构“IMAGE”的卤代酯在存在下 形成下述结构的次膦酸酯的有机碱，氢化上述酯以形成结构为重结晶的次膦酸的非对映体混合物，以回收优选的外消旋混合物，并使用拆分剂拆分，优选 形成相应的分解盐，其可以酸化成相应的酸。 此外，还提供了如上所述的酸和盐的新型中间体。

    Process for the preparation of 4-phosphinyl-3-keto-carboxylate and 4-phosphonyl-3-keto-carboxylate intermediates useful in the preparation of phosphorus containing HMG-COA reductase inhibitors
    9.
    发明授权
    Process for the preparation of 4-phosphinyl-3-keto-carboxylate and 4-phosphonyl-3-keto-carboxylate intermediates useful in the preparation of phosphorus containing HMG-COA reductase inhibitors 失效
    用于制备含磷HMG-COA还原酶抑制剂的4-氧膦基-3-酮羧酸酯和4-膦酰基-3-酮 - 羧酸酯中间体的方法

    公开(公告)号：US5349069A

    公开(公告)日：1994-09-20

    申请号：US171284

    申请日：1993-12-21

    申请人： John K. Thottathil ,  Wen S. Li

    发明人： John K. Thottathil ,  Wen S. Li

    IPC分类号： C07F9/30 ,  C07F9/32 ,  C07F9/572 ,  C07D209/12 ,  C07F9/02

    CPC分类号： C07F9/5728 ,  C07F9/301 ,  C07F9/3211 ,  C07F9/3294

    摘要： A process for the preparation of compounds of formula ##STR1## or salt thereof where R.sub.1 is --X--Z and X is --C.tbd.C--,R.sub.2 and R.sub.2 ' are independently hydrogen, alkyl or trialkylsilyl;R.sub.3 is hydrogen or alkyl; andZ is a hydrophobic anchor;which includes reacting a compound of formula ##STR2## where R.sub.4 is alkyl, cycloalkyl or aryl; and R.sub.5 is trialkylsilyl or triarylsilyl with a compound of formula ##STR3## where Y is a halogen, to form a compound of formula ##STR4## and hydrolyzing the compound of formula IV to obtain the compounds of formula I. Compounds of formula I or salt thereof where R.sub.1 is --OR.sub.2 ' may be prepared by reacting a compound of formula III with a compound of formulaP(OR.sub.2).sub.3. X

    摘要翻译： 制备式I的化合物或其盐的方法，其中R 1是-X-Z，X是-C 3 -C（O）C，R 2和R 2'独立地是氢，烷基或三烷基甲硅烷基; R3是氢或烷基; Z是疏水锚; 其包括使式（II）化合物与其中R 4为烷基，环烷基或芳基的化合物反应; 并且R 5是具有式III的化合物的三烷基甲硅烷基或三芳基甲硅烷基，其中Y是卤素，以形成式IV的化合物并水解式IV的化合物以获得式I的化合物。式I化合物 或其盐，其中R 1是-OR 2'可以通过使式III化合物与式P（OR 2）3的化合物反应来制备。 X