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    Carnitinamides of optically active aminoacids
    7.
    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

    申请人： Paolo De Witt ,  Maria O. Tinti

    发明人： Paolo De Witt ,  Maria O. Tinti

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

    CPC分类号： C07C237/12 ,  C07C323/58

    摘要： 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.

    摘要翻译： 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。