Abstract:
Quinolone derivs. of formula (I) are prepd. by reacting cpds. of formula (II) with EDTA in polar solvent(i.e. mixt. of water/MeOH and water/EtOH) in the presence of metal powder selected from a gp. of Zn, Cu, Mn or Fe and catalytic amt. of iodides(i.e. NaI, KI, CaI2) for 1-10 hr at 50-100 deg. C. In the formulas, R=H, Me, Et, propyl or butyl; X=Br; Z=Cl or piperazinyl gp.. (I) are useful as an antibacterial agent.
Abstract translation:喹诺酮衍生物。 式(I)的化合物是制备的。 通过cpds反应。 式(II)与EDTA在极性溶剂(即水/ MeOH和水/ EtOH的混合物)中在金属粉末存在下,选自gp。 的Zn,Cu,Mn或Fe和催化剂。 的碘化物(即NaI,KI,CaI 2)在50-100℃下1-10小时。 式中,R = H,Me,Et,丙基或丁基; X = Br的; Z = Cl或哌嗪基gp(I)可用作抗菌剂。
Abstract:
Title compds. (I)[R1=-CH3, -Cl, -Br, -NO2; R2=-H, -Cl; R3=-H, -CH3, - C(CH3)3, -Cl, -Br; R4=-H, Cl; R5=-H, -CH3, Cl, Br; R5=(II) , useful as a herbicide, were prepd. Thus, 0.66mol NaOH. and 0.299 mol 2,4,6- trichlorophenol in 450ml H2O were refluxed with 0.290 mol mono- chloro-acetate at 110-120≦̸C for 9-10 hrs and filtered. The precipitate was dissolved in 100g H2O, acidified with conc. HCl, and recrystallized with 90ml benzene to give 64.9g 2,4,6-trichlorophenoxy acetate (yield=85%).
Abstract:
The title (I)[R1=R, CH3, Cl, or Br; R2=H or Cl; R3=H, C(CH3)3, Cl or Br; R4=H or Cl; R5=H, CH3, Cl or Br; R6=SCH2, benzene, Cl, SC3H5 or SC4H9) are herbicides. Thus, a mixt. is given, contg. 150ml of benzene, 32.45g of 2,4,6-trichlorophenoxy acetyl chloride, 16.98ml of 4-chlorobenzylmercaptan and 23.1ml of triethylamine. In a decompression device, benzene and triethylamine are removed.
Abstract:
PURPOSE: Carbapenem derivatives and a preparation process thereof are provided, thereby preparing carbapenem derivatives having improved antimicrobial activity and renal dehydropeptidase I(DHP-I) stability. CONSTITUTION: Carbapenem derivatives represented by formula(I) are provided, wherein R1 and R2 are independently hydrogen, hydroxy substituted or unsubstituted C1 to C5 lower alkyl, or allyl, and form C3 to C6 heterocycle containing nitrogen and optionally hetero atoms of S or O together; and X is carbonyl or sulfonyl. A process for preparing the carbapenem derivatives of formula(I) comprises the steps of: reacting carbapenem scaffold of formula(II) with diphenylchloro phosphate or anhydrous trifluoromethane sulfonic acid in the presence of base and a solvent to prepare a carbapenem intermediate of formula(VII); reacting the carbapenem intermediate of formula(VII) with thiol derivative of formula(III) in the presence of base and a solvent to prepare a protected carbapenem derivative of formula(VIII); and hydrogenating the protected carbapenem derivative of formula(VIII) in the presence of a catalyst to remove a protecting group, wherein R3 is para-nitrobenzyl or allyl; R4 is para-nitrobenzyloxycarbonyl or allyoxycarbonyl; X is carbonyl or sulfonyl; and Y is -OPO(OPh)2 or -OSO2CF3.
Abstract:
본 발명은 항균제로 유용한 신규의 1-베타메틸카바페넴 유도체, 그를 포함하는 약학적 조성물 및 그의 제조방법에 관한 것으로서, 구체적으로 화학식 1로 표시되는 카바페넴 모핵의 2번 위치에 주요 관능기로서 5'-이소옥사졸로피롤리딘-3'-일티오기가 치환된 1-베타메틸카바페넴 유도체, 그를 포함하는 약학적 조성물 및 그의 제조방법에 관한 것이며, 본 발명에 의한 1-베타메틸카바페넴 유도체는 디히드로펩티다제-I에 대해 안정하고 그람양성균 및 그람음성균 모두에 대해 우수한 항균 활성을 보이는 유용한 항균제이다.
Abstract:
PURPOSE: Provided are a novel 1-β-methylcarbapenem derivative useful as antibiotics, its pharmaceutically acceptable salt, its manufacturing method and a pharmaceutical composition. containing it. CONSTITUTION: 1-β-methylcarbapenem derivative is represented by the formula(1), wherein R is represented by formulae; X is trifluormethyl or C1-C3 alkyl; Y is C1-C3 linear or branched aliphatic alkyl, C1-C3 sulfonamido alkyl in which one or two C1-C3 alkyl groups are substituted, C1-C3 alkyl substituted or unsubstituted C1-C3 carbo amidoalkyl group, C1-C3 hydroxyalkyl group, and C1-C3 alkyl substituted C1-C3 aminoalkyl or aryl; and Z is C1-C3 alkyl group.
Abstract:
본 발명은 일반식( I )로 표시되는 신규한 아지리딘기를 함유한 아조염료의 제조 및 이를 사용한 화학섬유, 특히 폴리에스테르, 폴리아미드 등 섬유의 염색방법에 관한 것이다. 본 발명은 일반식( I )로 표시되는 신규한 아지리딘기를 함유한 아조염료는 일반식( II )로 표시되는 N-메탄술포닐에틸아조 염료를 고리화하여 제조한다.
일반식( I )에 있어서, R 1 또는 R 2 가 각각 수소, 탄소 수 1 ∼ 5개의 알킬기, 알콕시, 아릴기 또는 아닐옥시기를 표시하며, D는 벤젠계, 티아졸계, 티아디아졸계, 티오펜계 또는 벤조티아졸계 유도체를 표시한다.