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    Carnitinamides of optically active aminoacids
    4.
    发明授权
    Carnitinamides of optically active aminoacids 失效
    光学活性氨基酸的肉碱酰胺

    公开(公告)号：US4343947A

    公开(公告)日：1982-08-10

    申请号：US220492

    申请日：1980-12-29

    Applicant: Paolo De Witt ,  Maria O. Tinti

    Inventor： Paolo De Witt ,  Maria O. Tinti

    IPC: A61K20060101 ,  A61K31/16 ,  A61K31/205 ,  C07C20060101 ,  C07C237/12 ,  C07C323/25 ,  C07D233/58 ,  C07D233/64 ,  C07C101/26 ,  C07C101/30 ,  C07C101/32

    CPC classification number: C07C237/12 ,  C07C323/58

    Abstract: Amides of carnitine or acyl-carnitines having general formula: ##STR1## wherein X.sup.- is a halogen anion, e.g. the chloride anionR is either hydrogen or an acyl radical, such as acetyl, propionyl or butyryl; andY is the residue of an optically active esterified amino-acid (e.g. the residue of L-phenylglycine methyl ester, ##STR2## are prepared by either (a) directly condensing D,L-carnitine (or acyl-D,L-carnitine) with an ester of an optically active aminoacid, or (b) preparing the acid halogenide of D,L-carnitine or acyl-D,L-carnitine and subsequently condensing it with an ester of an optically active aminoacid.The mixture of the diastereoisomer amides thus obtained is resolved by fractional crystallization from organic solvents into the respective separated diastereoisomers.These optically active amides are useful therapeutic agents for treating cardiac disorders, hyperlipidaemias and hyperlipoproteinaemias and, furthermore, can be hydrolyzed with procedures known per se into L-carnitine and D-carnitine, respectively.

    Abstract translation: 具有以下通式的肉碱或酰基肉碱的酰胺：其中X是卤素阴离子，例如， 氯离子R是氢或酰基，如乙酰基，丙酰基或丁酰基; 并且Y是光学活性酯化氨基酸的残基（例如，L-苯基甘氨酸甲酯的残基，通过以下方法制备：（a）直接冷凝D，L-肉毒碱（或酰基-D，L-肉毒碱 ），或（b）制备D，L-肉碱或酰基-D，L-肉毒碱的酰卤，然后将其与光学活性氨基酸的酯缩合，非对映异构体的混合物 这些光学活性酰胺是治疗心脏疾病，高脂血症和高脂蛋白血症的有用治疗剂，此外，可以用本身已知的方法将其水解成L-肉碱和 D-肉碱分别。

    Stereospecific hydrolysis of optically active esters
    7.
    发明授权
    Stereospecific hydrolysis of optically active esters 失效
    光学活性酯的立体特异性水解

    公开(公告)号：US06593478B2

    公开(公告)日：2003-07-15

    申请号：US10168792

    申请日：2002-06-24

    Applicant: Oreste Piccolo ,  Roberto Castagnani ,  Paolo De Witt

    Inventor： Oreste Piccolo ,  Roberto Castagnani ,  Paolo De Witt

    IPC: C07D30706

    CPC classification number: C07D307/33 ,  C07C227/32 ,  C07D307/20 ,  C07C229/22

    Abstract: A new, more efficient and highly stereospecific process is described for the preparation of compounds with general formula (R)-(I) and of absolute configuration (R), where the groups M, W, Q and Q1 are as defined in the description, starting from compounds of absolute configuration (S) by hydrolysis, in the presence of acids, of the corresponding esterified derivatives. The (R)-(I) products obtained with the process described herein are chiral synthons useful for the production of enanthiomerically pure drugs. The preparation of (R)-carnitine is also provided.

    Abstract translation: 描述了制备具有通式（R） - （I）和绝对构型（R）的化合物的新的，更有效和高度立体定向的方法，其中基团M，W，Q和Q 1如说明书中所定义 从具有相应酯化衍生物的酸存在下通过水解的绝对构型（S）化合物开始。 通过本文所述的方法获得的（R） - （I）产物是可用于生产精神药物的手性合成物。 还提供了（R） - 肉碱的制备。

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