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2. 发明公开

KR1020070056601A 신규한 플라본 유도체, 그의 제조 방법 및 이를 포함하는뇌신경계 질환의 예방 및 치료용 조성물 失效
标题翻译：新型FLAVONE衍生物，其制备方法及其含有预防和治疗脑神经系统疾病的组合物
公开(公告)号：KR1020070056601A
公开(公告)日：2007-06-04
申请号：KR1020050115501
申请日：2005-11-30
申请人： 한국과학기술연구원
发明人： 이용섭 , 진창배 , 김형자 , 김승환
IPC分类号： C07D311/30
摘要： A novel flavone derivative is provided to show excellent antioxidative effect, neuron protecting effect and neuroethological effect, thereby being usefully used for preventing and treating various neurodegenerative diseases such as stroke, chronic degenerative disease, Parkinson's disease and Alzheimer's disease. The flavone derivative is represented by the formula(1), wherein R1 is H or C1-4 alkoxy, R2 is H or hydroxy, each R3 and R4 is independently H or R5, R5 is glucose or -(CH2)mR6(m is from 0 to 3), and R6 is tetrahydrobenzopyran, tetrahydrobenzopyranylalkylacetate or tetrahydrobenzopyranylalkoxyalkyl substituted by at least one substituent selected from the group consisting of C3-7 heterocyclic compound including at least one of N and O; amino which is substituted or unsubstituted by at least one C1-4 alkyl; hydroxy; and hydroxyalkyl. The method for preparing the flavone derivative according to the reaction formula(1) comprises the steps of: (a) synthesizing a compound represented by the formula(VI) from a compound of the formula(I); and (b) after introducing at least one amine or glucose into the compound of the formula(VI) to prepare a compound represented by the formula(VII), deprotecting the compound of the formula(VII) to synthesize the compound of the formula(1). In the reaction formula(1), each R1 to R6 is same as defined above, X is halogen or alkyl halogen, MOM is methoxymethyl, and Bn is benzyl.
摘要翻译：提供了一种新型的黄酮衍生物，以显示优异的抗氧化作用，神经元保护作用和神经听觉效果，从而有效地用于预防和治疗各种神经变性疾病如中风，慢性退行性疾病，帕金森病和阿尔茨海默病。黄酮衍生物由式（1）表示，其中R1是H或C1-4烷氧基，R2是H或羟基，R3和R4独立地是H或R5，R5是葡萄糖或 - （CH2）mR6（m是 0至3），R6为四氢苯并吡喃基烷基乙酸酯或四氢苯并吡喃基烷氧基烷基，其被至少一个选自由以下组成的组的C3-7杂环化合物所取代：包括N和O中至少一个的杂环化合物; 被至少一个C 1-4烷基取代或未取代的氨基; 羟基; 和羟烷基。根据反应式（1）制备黄酮衍生物的方法包括以下步骤：（a）由式（I）化合物合成由式（VI）表示的化合物; 和（b）在将至少一种胺或葡萄糖引入式（VI）化合物中以制备式（Ⅶ）表示的化合物之后，将式（Ⅶ）化合物脱保护，合成式 1）。在反应式（1）中，每个R 1至R 6与上述定义相同，X为卤素或烷基卤素，MOM为甲氧基甲基，Bn为苄基。

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