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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。

    Selective processes for fosinopril polymorphs
    3.
    发明授权
    Selective processes for fosinopril polymorphs 失效
    福辛普利多选择选择性方法

    公开(公告)号：US5162543A

    公开(公告)日：1992-11-10

    申请号：US481009

    申请日：1990-02-16

    申请人： John A. Grosso

    发明人： John A. Grosso

    IPC分类号： A61K31/66 ,  A61P9/12 ,  C07F9/572

    CPC分类号： C07F9/5721

    摘要： Described herein is a process for selectively preparing and interconverting polymorph salts of fosinopril, an antihypertensive agent that inhibits angiotensin converting enzyme. Each polymorph is prepared by mixing an alkali metal carrier, fosinopril, water and a keto and/or hydroxylic solvent and isolating the polymorph formed from the reaction mixture. The less exothermic polymorph A is formed when the water makes up more than about 0.2% of the water and solvents; at about 0.2% or less, the more exothermic polymorph B is formed.

    Apparatus for alignment of workpieces
    5.
    发明授权
    Apparatus for alignment of workpieces 失效
    用于对准工件的装置

    公开(公告)号：US5249343A

    公开(公告)日：1993-10-05

    申请号：US749033

    申请日：1991-08-23

    申请人： John A. Grosso ,  Reena G. Malangone ,  John J. Masten, Jr. ,  Richard M. Schroedl ,  Robert Stokrocki ,  Donald G. Will

    发明人： John A. Grosso ,  Reena G. Malangone ,  John J. Masten, Jr. ,  Richard M. Schroedl ,  Robert Stokrocki ,  Donald G. Will

    IPC分类号： B23Q16/04 ,  B25B11/00 ,  B25B27/14

    CPC分类号： B23Q16/04 ,  B25B11/005 ,  Y10T29/53191 ,  Y10T29/53974 ,  Y10T29/53978

    摘要： An apparatus is provided for positioning a workpiece with high accuracy and repeatably positioning the workpiece with similar accuracy while avoiding further manual alignment operations. Tapered pins, movable axially against a spring, are used to support a registration frame above the workpiece and allow attachment of the registration frame to the workpiece with high accuracy after initial manual positioning of the workpiece. After attachment of the registration frame to the workpiece, the use of similar, spring-loaded, tapered pins assures accuracy of positioning without further manual alignment. The axial motion of the pins is particularly advantageous during alignment of a plurality of workpieces in stacks and for processes requiring two-sided registration. During the alignment operation, a vacuum block is relatively movable on a base block and a workpiece immobilized on the vacuum block by a vacuum selectively applied to a portion thereof. When correct alignment has been achieved, the vacuum block is immobilized while the registration frame is attached by selective application of a vacuum to another portion of the vacuum block.

    摘要翻译： 提供了一种设备，用于以高精度定位工件并以相似的精度重复地定位工件，同时避免进一步的手动对准操作。 在弹簧上轴向移动的锥形销用于支撑工件上方的配准框架，并允许在初始手动定位工件之后以高精度将配准框架附接到工件。 在将配准框架安装到工件后，使用类似的弹簧加载的锥形销确保定位的准确性，而无需进一步的手动对准。 在堆叠中的多个工件的对准期间以及需要双面配准的过程中，销的轴向运动是特别有利的。 在对准操作期间，真空块通过选择性地施加到其一部分上的真空而在基块和固定在真空块上的工件上相对移动。 当已经实现了正确的对准时，通过选择性地将真空吸附到真空块的另一部分而将配准框固定在一起固定真空块。