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    • 6. 发明公开
    • 신규 칼릭스[4]아렌 크라운 아자크라운 에테르 이합체및 이의 제조방법
    • 二手CALIX(4)具有三个金属离子识别位点的已知的AZACROWN ETHERE,并被用作提取溶剂及其制备方法
    • KR1020040110592A
    • 2004-12-31
    • KR1020030039949
    • 2003-06-19
    • 한국원자력연구원한국수력원자력 주식회사
    • 권선길이일희김종승
    • C07D493/18
    • PURPOSE: Dimeric calix(4)crown azacrown ether and a preparation method thereof are provided. The compound has three metallic ion-recognition sites, so that it can be useful as an extracting solvent of metallic ion. CONSTITUTION: The dimeric calix(4)crown azacrown ether having three metallic ion-recognition sites is represented by the formula(1), wherein n is an integer from 0 to 3; and R is hydrogen or C1-C10 alkyl. The method for preparing the dimeric calix(4)crown azacrown ether of the formula(1) comprises the steps of: (a) reacting a compound of the formula(I) with a compound of the formula(II) in the presence of cesium carbonate to prepare a compound of the formula(III); (b) modifying the compound of the formula(III) with a good leaving group to prepare a compound of the formula(IV); (c) reacting the compound of the formula(IV) with a compound of the formula(V) in the presence of cesium carbonate to prepare a compound of the formula(VI); (d) modifying the compound of the formula(VI) with a good leaving group to prepare a compound of the formula(VII); (e) reacting the compound of the formula(VII) with para-toluenesulfonamide in the presence of potassium carbonate to prepare a compound of the formula(VIII); and (f) deprotecting a tosylate group in the compound of the formula(VIII) in the presence of sodium/mercury amalgam and dibasic sodium phosphate, wherein the leaving group is tosylate or mesyl.
    • 目的:提供二甲基杯(4)冠azacrown醚及其制备方法。 该化合物具有三个金属离子识别位点,因此可用作金属离子的提取溶剂。 构成:具有三个金属离子识别位点的二聚杯(4)冠三氮烯醚由式(1)表示,其中n为0至3的整数; 和R是氢或C 1 -C 10烷基。 制备式(1)的二聚杯(4)冠阿扎洛韦醚的方法包括以下步骤:(a)使式(I)化合物与式(II)化合物在铯存在下反应 碳酸酯以制备式(III)化合物; (b)用良好的离去基团修饰式(III)的化合物以制备式(IV)的化合物; (c)在碳酸铯存在下使式(Ⅳ)化合物与式(Ⅴ)化合物反应制得式(Ⅵ)化合物; (d)用良好的离去基团修饰式(VI)的化合物以制备式(VII)的化合物; (e)使式(VII)化合物与对甲苯磺酰胺在碳酸钾存在下反应,制备式(Ⅷ)化合物; 和(f)在钠/汞汞齐和磷酸氢二钠的存在下使式(VIII)化合物中的甲苯磺酸酯基脱保护,其中离去基团是甲苯磺酸酯或甲磺酰基。
    • 7. 发明授权
    • 항 말라리아 아르테미시닌 유도체
    • 抗真菌药物衍生物
    • KR100131997B1
    • 1998-04-17
    • KR1019940015216
    • 1994-06-29
    • 김수언
    • 김수언
    • C07D493/18
    • Artemisinic acid is reacted with diazomethane in diethylether for esterifying the carboxyl group on 12 position of artemisinic acid to give methyl artemicinate, which is dissolved in prototropic solvent and electrophilic compound dissolved in prototropic solvent is added to it for introducing hydrogen on 11 position and the prototropic functional group on 13 position. The obtained methyl 11-hydro-13-X-artemisinate(X is cyan, amine, thioether, carboxyl, amide, or ether) is converted to 11-hydro-13-X-artemisinin(VII) by the conventional -lactonization.
    • 在二乙醚中使青蒿酸与重氮甲烷反应,酯化青蒿酸12位上的羧基,得到溶于原生质体溶剂中的青蒿酸甲酯,加入溶解在合成原溶剂中的亲电子化合物,将其引入11位,将原酸 功能组13位。 通过常规的β-乳化将得到的11-氢13-X-青蒿琥酯(X为青色,胺,硫醚,羧基,酰胺或醚)转化为11-氢-13-X-青蒿素(VII)。