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    • 7. 发明授权
    • N-(4-니트로/시아노 페닐티오카바모일)-L-아스파틸-L-페닐알라닌메틸에스테르의 제조방법
    • 制备N-(4-硝基/氰基苯基)羰基甲酰基-L-氨基甲酰基-L-苯甲酰甲基丙烯酸酯的方法
    • KR1019890000641B1
    • 1989-03-22
    • KR1019860000888
    • 1986-02-08
    • 씨제이 주식회사
    • 김진완이재흥유무영이상무
    • C07K5/06
    • The title cpds. (I)[X is a gp. contg. at least one unshared electron pair; R=alkyl), useful as an artificial sweetner, were prepd. Thus, β-benzyl-L-aspartic acid and Na2CO3 in H2O was reacted with 4-cyanophenylthiocyanate in EtOH for 24hr at room temp. to give 93% N-(4-cyanophenylcarbamoyl) β-benzyl-L-aspartic acid (II), which was condensated with L-phenylalaninemethylester. HCO in dioxane in the presence of DCC to give 95% N-(4-cyanophenylthiocarbamoyl)- β-benzyl- L-aspartyl-L-phenylalaninemethylester (II). 5.4g (II) in 100ml MeOH was hydrogenated over 10% Pd/C for 6hr at 20≦̸C and filtered. The filtrate was vacuum-concd. and adjusted to pH 4.5 with 1N HCl to give 98% (I)[X=cyano, R=Me).
    • 标题cpds。 (I)[X是gp。 contg。 至少一个非共享电子对; R =烷基),可用作人造甜味剂。 因此,将H 2 O中的β-苄基-L-天冬氨酸和Na 2 CO 3与EtOH中的4-氰基苯基硫氰酸酯在室温下反应24小时。 得到93%N-(4-氰基苯基氨基甲酰基)β-苄基-L-天冬氨酸(II),其与L-苯丙氨酸甲酯缩合。 HCO在二恶烷中,在DCC存在下,得到95%N-(4-氰基苯基硫代氨基甲酰基)-β-苄基-L-天冬氨酰基-L-苯丙氨酸甲酯(II)。 C,并通过10%Pd / C将5.4g(II)的100ml MeOH溶液在20℃下氢化6小时并过滤。 滤液真空浓缩。 并用1N HCl调节至pH 4.5,得到98%(I)[X =氰基,R = Me]。
    • 9. 发明授权
    • 신규한 베타락탐 항생물질 및 이의 제조방법
    • 苯并噻嗪衍生物喹诺酮
    • KR1019970004041B1
    • 1997-03-24
    • KR1019880017627
    • 1988-12-28
    • 씨제이 주식회사
    • 조성기이상무김천규
    • C07D499/44
    • Novel beta-LACTAME which appears antibacterial activity not only to gram-positive bacteria but also to gram-negative bacteria and pseudomonas, and has good solubility is disclosed in this invention. 1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7-(4-formyl-1-piperazinyl) quinolin-3-carboxylic acid and triethylamine is admixed to dried dichloromethane, thereafter, ethylchloroformate is added. Then, D-a-amino- p-hydroxy benzyl penicillin and triethylamine dissolved in dried dimethylformamide are admixed to yield beta-lactame of general formula(I).
    • 在本发明中公开了新颖的β-LACTAME,其不仅对革兰氏阳性细菌,而且对革兰氏阴性细菌和假单胞菌具有抗菌活性,并且具有良好的溶解性。 1-环丙基-6-氟-1,4-二氢-4-氧代-7-(4-甲酰基-1-哌嗪基)喹啉-3-羧酸和三乙胺混合到干燥的二氯甲烷中,然后加入氯甲酸乙酯。 然后将D-α-氨基对羟基苄基青霉素和溶解在干燥的二甲基甲酰胺中的三乙胺混合,得到通式(I)的β-内酰胺。