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    • 2. 发明公开
    • 신규 1-베타메틸카바페넴 유도체 및 그의 제조방법
    • 新型1-甲基胆碱衍生物及其制备方法
    • KR1020020005334A
    • 2002-01-17
    • KR1020000039375
    • 2000-07-10
    • 한국과학기술연구원
    • 김동진박상우신계정유경호강용구
    • C07D477/10
    • PURPOSE: Provided is a novel 1-β- methylcarbapenem derivative which has an antibacterial effect on both gram negative and positive bacteria and stability to dihydropeptidase-I, and is thus useful as antibacterial agent. And a pharmaceutical composition containing it and its manufacturing method are also provided. CONSTITUTION: The novel 1-β- methylcarbapenem derivative is represented by the formula(I), wherein R is described as in the description, X is ethoxycarbonyl group or hydroxymethyl group; Y is hydroxymethyl group or ethoxycarbonyl group; and Z is methyl group or carbamoylmethyl group. Its manufacturing method comprises the steps of: reacting enolphosphate with thiol derivative in the presence of base, in appropriate solvent to prepare protected carbapenem derivative; and deprotecting the protected carbapenem derivative to obtain 1-β- methylcarbapenem derivative.
    • 目的:提供一种新型的1-β-甲基碳青霉烯衍生物,对革兰阴性和阳性细菌具有抗菌作用,对二氢肽酶-I具有稳定性,因此可用作抗菌剂。 还提供含有它的药物组合物及其制备方法。 构成:新颖的1-β-甲基碳青霉烯衍生物由式(I)表示,其中R如描述中所述,X是乙氧基羰基或羟甲基; Y是羟甲基或乙氧基羰基; Z为甲基或氨基甲酰基甲基。 其制造方法包括以下步骤:在碱的存在下,在合适的溶剂中使烯醇化磷酸酯与硫醇衍生物反应,制备保护的碳青霉烯衍生物; 并将保护的碳青霉烯衍生物脱保护得到1-β-甲基碳青霉烯衍生物。
    • 7. 发明公开
    • 메로페넴 삼수화물의 제조방법
    • 制备三聚氰胺的方法
    • KR1020110062515A
    • 2011-06-10
    • KR1020090119263
    • 2009-12-03
    • (주)하이텍팜
    • 문한서김영훈구영삼김정수
    • C07D477/20C07D477/10C07D403/12A61P31/00
    • PURPOSE: A method for preparing meropenem trihydrate with high yield and high purity is provided to cheaply and easily prepare meropenem trihydrate in a commercial scale. CONSTITUTION: A method for preparing meropenem trihydrate comprises: a step of performing substitution reaction of a compound of chemical formula II and a compound of chemical formula III in a mixture solvent containing low polar organic solvent of acetone, tetrahydrofuran, or acetonitrile and high polar organic solvent of N-methyl-pyrrolidinone, N,N-dimethylformamide, or N,N-dimethylacetate amide under the presence of a base to prepare a compound of chemical formula IV; a step of deprotecting the compound of chemical formula IV in the mixture solvent in situ; and a step of adding an organic solvent of acetone, tetrahydrofuran, acetonitrile, ethanol, or propanol.
    • 目的:提供一种以高产率和高纯度制备三烯酸美罗培南的方法,以便以商业规模便宜地并且容易地制备三油菊烯酸。 构成:制备美罗培南三水合物的方法包括:将化学式II化合物和化学式III的化合物在含有丙酮,四氢呋喃或乙腈的低极性有机溶剂和高极性有机溶剂的混合溶剂中进行取代反应的步骤 N-甲基 - 吡咯烷酮,N,N-二甲基甲酰胺或N,N-二甲基乙酸酯酰胺的溶剂,以制备化学式IV的化合物; 在混合溶剂中原位化学式IV化合物脱保护的步骤; 和加入丙酮,四氢呋喃,乙腈,乙醇或丙醇的有机溶剂的步骤。