Stereoselective synthesis of 2-hydroxy-4-phenylbutyric acid esters
    3.
    发明申请
    Stereoselective synthesis of 2-hydroxy-4-phenylbutyric acid esters 失效
    2-羟基-4-苯基丁酸酯的立体选择性合成

    公开(公告)号:US20040236141A1

    公开(公告)日:2004-11-25

    申请号:US10719660

    申请日:2003-11-21

    CPC classification number: C07C67/22 Y02P20/55 C07C69/732

    Abstract: A process is described for the stereospecific preparation of an ester of formula (I): wherein * signifies the (R) stereoisomer; R1 is selected from C1-6 alkyl, preferably ethyl; and R2 is hydrogen, a protecting group or a leaving group which process comprises reaction of a nitrile of formula (II): wherein * signifies the (R) stereoisonomer; and Ph is the phenyl group C6 H5 with a solution of an inorganic acid in an alcohol and optional conversion of the compound of formula (I) wherein R2 is H so prepared to any other desired compound of formula (I) by standard methods in the art. The compounds of formula (I) are chiral esters, useful as intermediates in the synthesis of the family of acetylcholine esterase (ACE) inhibitors known as nullprilsnull, such as lisinopril, cilazapril, enalapril, benazepril, ramipril, delapril, enalaprilat, imidapril, spirapril, trandolapril and others.*Ph-CH2nullCH2nullCH(OR2)nullCOOR1nullnull(I)*Ph-CH2nullCH2nullCH(OH)nullCNnullnull(II)

    Abstract translation: 描述了式(I)的酯的立体特异性制备的方法:其中*表示(R)立体异构体; R 1选自C 1-6烷基,优选乙基; 并且R 2是氢,保护基团或离去基团,该方法包括式(II)的腈的反应:其中*表示(R)立体异构体; Ph是苯基C6H5,其中无机酸在醇中的溶液,并且任选地将其中R 2为H的式(I)化合物转化为任何其它所需的式(I)化合物,通过标准 本领域的方法。 式(I)化合物是手性酯,可用作合成称为“prils”的乙酰胆碱酯酶(ACE)抑制剂家族的中间体,例如赖诺普利,西拉普利,依那普利,贝那普利,雷米普利,地拉普利,依那普利拉,咪达匹尔 ,咯普利,群多普利等。 * Ph-CH 2 -CH 2 -CH(OR 2)-COOR 1(I)* Ph-CH 2 -CH 2 -CH(OH)-CN(II)

    Process for converting nitriles to carboxylic esters
    6.
    发明授权
    Process for converting nitriles to carboxylic esters 失效
    将腈转化为羧酸酯的方法

    公开(公告)号:US4450112A

    公开(公告)日:1984-05-22

    申请号:US325028

    申请日:1981-11-25

    CPC classification number: C07C67/22

    Abstract: Reaction of a nitrile, an alcohol and water in the presence of a catalyst comprising rhodium, iridium or platinum complexed with hydroxo and tertiary phosphine moieties, to produce the corresponding carboxylic ester.

    Abstract translation: 在含有铑,铱或与氢和叔膦部分配位的铂的催化剂存在下,腈,醇和水的反应,以产生相应的羧酸酯。

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