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    • 51. 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。
    • 52. 发明授权
    • 옥사졸리논계 유도체 및 그의 제조방법과 용도
    • 氧杂环丁烷衍生物及其制备方法和用途
    • KR100125130B1
    • 1997-12-05
    • KR1019940020300
    • 1994-08-17
    • 한국과학기술연구원
    • 박상우신계정김동찬
    • C07D413/02A01N43/26C07D263/22
    • C07D413/04A01N43/76C07D263/42
    • The oxazolinon type derivative represented by the following general formula(I) and its preparing method is disclosed with uses as herbicides wherein, R is low alkyl or halogen, low alkyl or trifluoromethyl containing phenyl, X is the same or different, halogen, carbomethoxy, nitro, or halogen, trifluoro substituted phenoxy, A is nitrogen, carbon, n is an integer of 1-3. The oxazolinon type derivative is prepared by a condensation reaction of M-amino acid of the general formula(II) and an acid chloride of the general formula(III) to produce an amino substituted M-amino acid of the general formula(IV), and then dehydration reaction after subjecting to reacting with anhydride nitric acid. The herbicide according to this invention has excellent herbicidal effectiveness in treatment of pre- or postemergency against a dicotyledonous plant.
    • 公开了以下通式(I)表示的恶唑啉型衍生物及其制备方法,其用作除草剂,其中R为低级烷基或卤素,低级烷基或含三氟甲基的苯基,X为相同或不同的卤素,甲酯基, 硝基或卤素,三氟取代的苯氧基,A是氮,碳,n是1-3的整数。 恶唑啉型衍生物通过通式(II)的M-氨基酸与通式(III)的酰氯的缩合反应制备,得到通式(IV)的氨基取代的M-氨基酸, 然后与酸酐硝酸反应后进行脱水反应。 根据本发明的除草剂在对双子叶植物的芽前或芽后处理方面具有优异的除草效果。