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    • 3. 发明公开
    • 트리사이클로 화합물 당화 유도체
    • 甘氨酸三聚体化合物衍生物
    • KR1020130015838A
    • 2013-02-14
    • KR1020110078107
    • 2011-08-05
    • (주) 제노텍
    • 김재종우진석임시규강선엽김대희서원민양지영백승원주정훈이상미유상은이미옥이기호박병철
    • C07H7/06C07D498/14C12P19/00A61P37/06
    • PURPOSE: A method for preparing tricyclo compound derivatives of a novel structure is provided to obtain glycosylated derivatives with immunosuppression and to improve superior solubility. CONSTITUTION: A glycosylated tricyclo compound derivative is denoted by a chemical formula 1. The tricyclo compound is tacrolimus, ascomycin, rapamycin, or meridamycin. A linker is a formyl group, an acetyl group, a propionyl group, a butyl group, an acryl group, an ethylsuccinyl group, a succinyl group, or an aminohexyl group. A method for preparing the derivative of chemical formula 1 comprises: a step of introducing a succinyl group at 1 -OH site using glucose and introducing a protection group to -OH residue; a step of adding a macrolide compound to compound 25 and removing the R3 and R4 protection group from the compound 25.
    • 目的:提供一种新型结构的三环化合物衍生物的制备方法,以获得具有免疫抑制作用的糖基化衍生物,提高溶解度。 构成:糖化三环化合物衍生物由化学式1表示。三环化合物是他克莫司,子囊霉素,雷帕霉素或美里达霉素。 接头是甲酰基,乙酰基,丙酰基,丁基,丙烯酰基,乙基琥珀酰基,琥珀酰基或氨基己基。 制备化学式1的衍生物的方法包括:使用葡萄糖在1 -OH位置引入琥珀酰基并将保护基引入-OH残基的步骤; 向化合物25中加入大环内酯类化合物并从化合物25除去R3和R4保护基的步骤。