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ACYLATED ALCANOLAMIDES OF LYSERGINIC ACID DISPLAYING NEOTROPIC ACTIVITY

机译:麦角酸的酰基化酰胺具有新活性

摘要

Processes for the synthesis of acylated lysergic acid alkanolamides of the formula I, which can be used for the therapy of all sorts of forms of reduced cerebral ability, in particular the age-related manifestations, are described. The preparation of I is carried out according to the invention either by acylation of the lysergic acid diethanolamides IV or lysergic acid ethanolamides V occurring as intermediates in a conventional manner, for example by means of a reactive acid derivative in pyridine or by coupling of an appropriate lysergic acid II, which has previously been converted into an activated form, with an already acylated amine VII. Finally, I unsubstituted in the 2-position can be converted into 2-halogenated derivatives using a mild halogenating agent, such as, for example, N-bromosuccinimide in dichloromethane.
机译:描述了式I的酰化麦角酸链烷醇酰胺的合成方法,其可用于治疗各种形式的脑功能降低,特别是与年龄有关的表现。根据本发明,通过以常规方式酰化作为中间体存在的麦角酸二乙醇酰胺IV或麦角酸乙醇酰胺V来进行I的制备,例如通过在吡啶中的反应性酸衍生物或通过适当的偶联。麦角酸Ⅱ,它已经被酰化的胺预先转化成活化形式。最后,可以使用温和的卤化剂,例如二氯甲烷中的N-溴琥珀酰亚胺,将2-位上未取代的I转化为2-卤代衍生物。

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