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    • 9. 发明授权
    • Process for the preparation of monocyclic, bicyclic and tricyclic
aminoacids
    • 制备单环,双环和三环氨基酸的方法
    • US4691022A
    • 1987-09-01
    • US623200
    • 1984-06-21
    • Rainer HenningHansjorg Urbach
    • Rainer HenningHansjorg Urbach
    • C07D207/16C07D207/20C07D209/08C07D209/42C07D209/52C07D209/54C07D209/72C07D209/96C07C103/52
    • C07D209/54C07D207/16C07D207/20C07D209/08C07D209/42C07D209/52
    • The invention relates to a process for the preparation of compounds of the formula I ##STR1## in which R represents hydrogen, alkyl or aralkyl, and R.sup.1 to R.sup.6 denote identical or different radicals hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, cycloalkenylalkyl, aralkyl or aryl, both being monosubstituted, disubstituted or trisubstituted in the aryl moiety by alkyl, alkoxy, hydroxyl, halogen, nitro, methylenedioxy and/or cyano, or in which two of the radicals R.sup.1 to R.sup.6, together with the carbon atom(s) bearing them form a monocyclic or bicyclic ring system, and the remaining radicals are hydrogen, which process comprises converting, with an oxidizing agent in the presence of a silver salt, a pyrrolidine derivative of the formula II into a .DELTA..sup.1 -pyrroline derivative of the formula III, reacting the latter with hydrogen cyanide or a metal cyanide to form a nitrile of the formula IV, and subjecting the latter to solvolysis with a compound of the formula ROH.
    • 本发明涉及一种制备式I化合物的方法,其中R代表氢,烷基或芳烷基,R1至R6表示相同或不同的基团氢,烷基,环烷基,环烷基烷基,环烯基烷基,芳烷基或芳基 两者在芳基部分中被烷基,烷氧基,羟基,卤素,硝基,亚甲二氧基和/或氰基单取代,二取代或三取代,或其中两个基团R1至R6与带有它们的碳原子一起 形成单环或双环系统,其余基团是氢,该方法包括用银盐存在下的氧化剂将式II的吡咯烷衍生物转化为式III的DELTA 1-吡咯啉衍生物 使后者与氰化氢或金属氰化物反应以形成式IV的腈,并使其后者与式ROH的化合物溶剂解。
    • 10. 发明授权
    • N-Acyl hexahydroindole-2-carboxylic acids and anti-hypertensive use
thereof
    • N-酰基六氢吲哚-2-羧酸及其抗高血压用途
    • US4562202A
    • 1985-12-31
    • US477333
    • 1983-03-21
    • Hansjorg UrbachRainer HenningVolker TeetzHans WissmannReinhard Becker
    • Hansjorg UrbachRainer HenningVolker TeetzHans WissmannReinhard Becker
    • A61K31/403A61K31/404A61K31/405A61K38/00A61K38/55A61P9/12C07D209/42C07K1/02C07K1/113C07K5/02C07K5/06C07K14/81A61K31/40
    • C07K5/0222C07D209/42A61K38/00
    • The invention relates to compounds of the formula I ##STR1## in which n denotes 0 or 1,R denotes hydrogen, alkyl or aralkyl, R.sup.1 denotes hydrogen or alkyl, which can optionally be substituted by amino, acylamino or benzoylamino, alkenyl, cycloalkyl, cycloalkenyl, cycloalkylalkyl, aryl or partially hydrogenated aryl, which each can be substituted by alkyl, alkoxy or halogen, arylalkyl or aroylalkyl, both of which can be substituted in the aryl radical as defined in the aforegoing, a monocyclic or bicyclic sulfur or oxygen and/or nitrogen heterocyclic radical, or a side chain of a naturally occurring aminoacid, R.sup.2 denotes hydrogen, alkyl, alkenyl or arylalkyl, Y denotes hydrogen or hydroxyl, Z denotes hydrogen or Y and Z together denote oxygen and X denotes alkyl, alkenyl, cycloalkyl, aryl, which is monosubstituted, disubstituted or trisubstituted by alkyl, alkoxy, hydroxyl, halogen, nitro, amino, alkylamino, dialkylamino or methylenedioxy or 3-indolyl,and their physiologically acceptable salts, processes for their preparation, agents containing these and their use as medicaments and also bicyclic amino acids as their intermediates and processes for their preparation.
    • 本发明涉及式I的化合物,其中n表示0或1,R表示氢,烷基或芳烷基,R1表示氢或烷基,其可任选被氨基,酰氨基或苯甲酰基氨基取代, ,环烷基,环烯基,环烷基烷基,芳基或部分氢化的芳基,其各自可以被烷基,烷氧基或卤素,芳基烷基或芳酰基烷基取代,二者可以在如上所定义的芳基中被取代,单环或双环硫 或氧和/或氮杂环基或天然存在的氨基酸的侧链,R 2表示氢,烷基,烯基或芳烷基,Y表示氢或羟基,Z表示氢或Y,Z一起表示氧,X表示烷基, 烯基,环烷基,芳基,其被烷基,烷氧基,羟基,卤素,硝基,氨基,烷基氨基,二烷基氨基或亚甲二氧基或3-吲哚基单取代或三取代,及其生理学 表盐,其制备方法,含有这些物质的药剂及其作为药物的用途以及双环氨基酸作为其中间体及其制备方法。