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37 条记录 (耗时 0.036 秒)

    Process for preparing (trans)-4-phenyl-L-proline derivatives
    1.
    发明授权
    Process for preparing (trans)-4-phenyl-L-proline derivatives 失效
    制备（反式）-4-苯基-L-脯氨酸衍生物的方法

    公开(公告)号：US4912231A

    公开(公告)日：1990-03-27

    申请号：US209165

    申请日：1988-06-17

    申请人： David Kronenthal ,  Paula L. Kuester ,  Richard H. Mueller

    发明人： David Kronenthal ,  Paula L. Kuester ,  Richard H. Mueller

    IPC分类号： C07D207/16

    CPC分类号： C07D207/16 ,  Y02P20/55

    摘要： A process is provided for preparing (trans)-4-phenyl-L-proline derivatives with excellent stereospecificity, which are useful in preparing certain ACE inhibitors, which process involves reacting a proline derivative of the structure ##STR1## whereing R is a nitrogen protecting group, R.sub.1 is H, aryl, arylalkyl or lower alkyl, and X is a leaving group such as fluorine, an alkyl sulfonate, arylsulfonate or cycloalkyl sulfonate is reacted with an aromatic nucleophile, such as benzene, in the presence of a Lewis acid such as AlCl.sub.3 to form the (trans)-4-phenyl-L-proline derivative of the structure ##STR2##

    摘要翻译： 提供了制备具有优异立体定向性的（反式）-4-苯基-L-脯氨酸衍生物的方法，其可用于制备某些ACE抑制剂，该方法包括使结构“IMA”的脯氨酸衍生物反应，其中R为氮保护 基团，R 1是H，芳基，芳基烷基或低级烷基，X是离去基团如氟，烷基磺酸酯，芳基磺酸酯或环烷基磺酸酯与芳族亲核试剂例如苯在路易斯酸存在下反应， 作为AlCl 3以形成结构“（IMAGE）”的（反式）-4-苯基-L-脯氨酸衍生物

    Process for preparing (trans)-4-substituted-dl-proline derivatives
    2.
    发明授权
    Process for preparing (trans)-4-substituted-dl-proline derivatives 失效
    制备（反式）-4-取代-DL-脯氨酸衍生物的方法

    公开(公告)号：US4937355A

    公开(公告)日：1990-06-26

    申请号：US297522

    申请日：1989-01-17

    申请人： John Kloss ,  David Kronenthal ,  Christopher M. Cimarusti ,  Richard H. Mueller

    发明人： John Kloss ,  David Kronenthal ,  Christopher M. Cimarusti ,  Richard H. Mueller

    IPC分类号： C07D207/16

    CPC分类号： C07D207/16 ,  Y02P20/55

    摘要： A process is provided for preparing (trans)-4-phenyl-DL-proline derivatives, which are useful in preparing certain angiotensin converting enzyme inhibitors, which process involves reacting an ester of the structure ##STR1## wherein X is a leaving group such as tosylate, R.sup.3 is lower alkyl, R is cyclohexyl, phenyl or substituted phenyl, and R.sup.1a is a protecting group, with a potassium amide base such as potassium hexamethyldisilazide under reduced temperatures to form the trans-4-substituted proline ester derivative of the structure ##STR2## then hydrolyzing the proline ester to the acid of the structure ##STR3## and removing the R.sup.1a nitrogen protecting group to form the unprotected acid of the structure ##STR4##

    Preparation of boronic acid derivatives
    6.
    发明授权
    Preparation of boronic acid derivatives 失效
    硼酸衍生物的制备

    公开(公告)号：US5039795A

    公开(公告)日：1991-08-13

    申请号：US369390

    申请日：1989-06-21

    申请人： Richard H. Mueller

    发明人： Richard H. Mueller

    IPC分类号： C07B59/00 ,  C07F5/02 ,  C07F13/00

    CPC分类号： C07F5/025

    摘要： An improved process for preparation of compounds of the formula ##STR1## as disclosed. These compounds are useful as intermediates in the preparation of boronic acid adducts of technetium 99m dioxime complexes of the formula.sup.99m Tc X(Y).sub.3 Zwhich are useful as imaging agents.

    摘要翻译： 如所公开的，制备式“IMAGE”的化合物的改进方法。 这些化合物可用作制备99mTc X（Y）3Z锝99m二肟络合物的硼酸加合物的中间体，其可用作显像剂。