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1. 发明公开

KR1020000002400A [(아릴)이소옥소졸릴]메틸렌-아자비시클로 화합물 및 이의 제조방법 失效
标题翻译：（ARYL）ISOOXOZOLYL]甲基 - 偶氮化合物及其制造方法
公开(公告)号：KR1020000002400A
公开(公告)日：2000-01-15
申请号：KR1019980023118
申请日：1998-06-19
申请人： 한국과학기술연구원
发明人： 고훈영 , 장문호 , 김유승 , 최경일 , 조용서 , 배애님 , 차주환 , 공재양 , 천혜경 , 정대영
IPC分类号： C07D453/00 , C07D261/20
摘要： PURPOSE: The compound is provided which exhibits a high affinity for muscarinic acetylcholine receptor and is useful as therapeutic agent of cerebral nerve disease such as Alzheimer's disease. CONSTITUTION: The carbonyl compound of the formula (II), wherein, n is integer 1 or 2, is reacted with phosphonium salt compound of formula (III), in which R is H, halo, alkoxy, cyano, alkyl, alkenyl, alkinyl, hydroxy, amino, nitro, 4-methoxybenzyloxy, t-butoxycarbonylamino or its salt; R1, R2 and R3 are alkyl, aryl or aralkyl, respectively; X is halogen, or with phosphonate compound of the formula (IV) in the presence of solvent and base to give £(aryl) isooxozolyl| methylene-azabicyclo compound of the formula (I). Thus, 188mg of potassium t-butoxide and 482mg of diethyl 3-(4-methylphenyl)-5-isooxazolylmethylphosphonate being dissolved in tetrahydrofuran are stirred for 30 minutes at 22°C to give 3-£3-(4-methylphenyl)isooxazol-5-yl|methylene-1-azabicyclo£2.2.2|octane oxalic acid salt.
摘要翻译：目的：提供对毒蕈碱性乙酰胆碱受体具有高亲和力的化合物，并且可用作脑神经疾病如阿尔茨海默病的治疗剂。构成：其中n为1或2的式（II）的羰基化合物与式（III）的鏻盐化合物反应，其中R为H，卤素，烷氧基，氰基，烷基，烯基，炔基，羟基，氨基，硝基，4-甲氧基苄氧基，叔丁氧基羰基氨基或其盐; R1，R2和R3分别是烷基，芳基或芳烷基; X为卤素，或与式（IV）的膦酸酯化合物在溶剂和碱存在下反应，得到（芳基）异恶唑基| 式（I）的亚甲基 - 氮杂二环化合物。因此，将188mg叔丁醇钾和482mg 3-（4-甲基苯基）-5-异恶唑甲基膦酸二乙酯溶于四氢呋喃中，在22℃下搅拌30分钟，得到3- {3-（4-甲基苯基）异恶唑-4-基） 5-基|亚甲基-1-氮杂双环{2.2.2 |辛酸草酸盐。

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