Abstract:
PURPOSE: Provided is (±)-2-(4-chlorobenzoylamino)-3-(2(1H)-quinolinone-4-mono)propionic acid which is prepared through simplified processing steps at high yield and high purity. CONSTITUTION: 4-halomethyl-2(1H)-quinolinone(formula III) reacts with dialkyl 4-chlorobenzoylamino malonate(formula IV) in the presence of an inorganic base in an alcoholic solvent to prepare alkyl 2-(4-chlorobenzoylamino)-2-(alkoxycarbonyl)-3-(2(1H)-quinolinone-4-mono)propionate(formula II) as an intermediate. It selectively suffers decarboxylation and hydrolysis using an acids mixture wherein acetic acid is mixed with other acids in a volume ratio of 1:0.3-10.2, thereby preparing the (±)-2-(4-chlorobenzoylamino)-3-(2(1H)-quinolinone-4-mono)propionic acid(formula I). In the formulas, R is C1-6 alkyl group, and X1 is halogen.
Abstract:
PURPOSE: Provided is a process for producing a £2-(2,6-dichloroanilino)phenyl|acetoxy acetate (aceclofenac) being used for an antipyretic, an analgesic in a high purity and yield, which is an economical and safe process. CONSTITUTION: A aceclofenac (formula 1) is produced by hydrolyzing an ester of a 2,2,2-trihaloethyl ester £2-(2,6-dichloroanilino)phenyl|acetoxy acetate (formula 2) having two esters with Zn or Zn-Cu catalyst in a formic acid, an acetic acid or a trifluoro acetate at 30-60°C for 3-8 hrs. The compound (formula 2) is produced by reacting a sodium or potassium £2-(2,6-dichloroanilino)phenyl| acetate (diclofenac) and a trihaloethyl halo acetate in an equivalent ratio of 1:1.1-1.5 in a dimethyl formamide or a dimethyl sulfoxide at 30-50°C. In the formula, X is a halogen.
Abstract:
PURPOSE: Provided is (±)-2-(4-chlorobenzoylamino)-3-(2(1H)-quinolinone-4-mono)propionic acid which is prepared through simplified processing steps at high yield and high purity. CONSTITUTION: 4-halomethyl-2(1H)-quinolinone(formula III) reacts with dialkyl 4-chlorobenzoylamino malonate(formula IV) in the presence of an inorganic base in an alcoholic solvent to prepare alkyl 2-(4-chlorobenzoylamino)-2-(alkoxycarbonyl)-3-(2(1H)-quinolinone-4-mono)propionate(formula II) as an intermediate. It selectively suffers decarboxylation and hydrolysis using an acids mixture wherein acetic acid is mixed with other acids in a volume ratio of 1:0.3-10.2, thereby preparing the (±)-2-(4-chlorobenzoylamino)-3-(2(1H)-quinolinone-4-mono)propionic acid(formula I). In the formulas, R is C1-6 alkyl group, and X1 is halogen.
Abstract:
본 발명은 해열제, 골관절염 및 류마티스관절염 등의 관절질환과 각종 통증에 우수한 치료 효과를 나타내는 소염진통제로 널리 알려져 있는 화학식 1의 화합물[관용명:아세클로페낙(Aceclofenac)]의 신규 제조방법 및 그 제조 과정에서 중간체로 사용되는 화학식 2의 화합물 및 그의 제조방법에 관한 것이다:
상기식에서, R 1 은 C 1-4 알킬렌이고 R 2 는 C 1-4 알킬이다. 본 발명은 매우 저렴하고 사용이 편리한 산(acid)을 사용하여 선택적으로 가수분해시킴으로써 고수율 및 고순도의 화학식 1의 아세클로페낙을 간편하게 제조할 수 있다.
Abstract:
PURPOSE: An immune enhancer is provided to be used as an antibiotic and an anti-cancer medicine separately or mixed with another ingredient. CONSTITUTION: An immune enhancer containing a lombricine as an effective ingredient activates an immuno-cell of an organism for having an effect of enhancing an immune of the organism. The immune enhancer may be used as an antibiotic and an anti-cancer medicine separately or by mixed with other antibiotic or anti-cancer medicine for minimizing a virulence and maximizing an effect.
Abstract:
본 발명은 간흡충, 폐흡충, 유구낭미충 및 고충(Sparganum) 감염증을 동시에 진단할 수 있는 효소면역진단(ELISA: Enzyme-Linked ImmunoSorbent Assay) 키트에 관한 것이다. 본 발명의 키트를 이용하면, 주요 조직내 기생충 감염증을 한 번에 규격화된 방법으로 간편하고 신속·정확하게 진단할 수 있다.
Abstract:
PURPOSE: Provided is a process for preparing amorphous form of cefuroxime axetil, thereby producing amorphous form of cefuroxime axetil, which is excellent in elution in a living body and has stability, in high yield and purity. CONSTITUTION: The amorphous cefuroxime axetil represented by the formula(1) is manufactured by the steps of: dissolving cefuroxime axetil in a polar organic solvent; passing CO2 gas therethrough; and adding a water soluble solution containing inorganic salts to precipitate amorphous cefuroxime axetil.
Abstract:
PURPOSE: An enzyme-linked immunosorbent assay kit of Clonorchis sinensis., Paragonimus westermani, Cysticerus cellulosae and Sparganum infection syndrome is provided, thereby rapidly and correctly diagnosing the infection of main tissues with parasites. CONSTITUTION: The enzyme-linked immunosorbent assay kit of Clonorchis sinensis., Paragonimus westermani, Cysticerus cellulosae and Sparganum infection syndrome comprises a multi-well microplate or strip containing antigens of Clonorchis sinensis. Paragonimus westermani, Cysticerus cellulosae and Sparganum; a human serum which doesn't react with the antigens of Clonorchis sinensis. Paragonimus westermani, Cysticerus cellulosae and Sparganum as a negative standard serum; and a human serum which specifically and independently reacts with the antigens of Clonorchis sinensis., Paragonimus westermani, Cysticerus cellulosae and Sparganum as a positive standard serum.
Abstract:
PURPOSE: Provided is a process for preparing amorphous form of cefuroxime axetil, thereby producing amorphous form of cefuroxime axetil, which is excellent in elution in a living body and has stability, in high yield and purity. CONSTITUTION: The amorphous cefuroxime axetil represented by the formula(1) is manufactured by the steps of: dissolving cefuroxime axetil in a polar organic solvent; passing CO2 gas therethrough; and adding a water soluble solution containing inorganic salts to precipitate amorphous cefuroxime axetil.
Abstract:
PURPOSE: Provided is a pharmaceutical composition for intramuscular injection containing loxoprofen having excellent anti-inflammatory effects, as an active ingredient, and its pharmaceutically acceptable salts. CONSTITUTION: The pharmaceutical composition for intramuscular injection contains loxoprofen represented by the formula(1) or its pharmaceutically acceptable salts. It is manufactured by dissolving loxoprofen or its pharmaceutically acceptable salt, a stabilizing agent or solution adjuvant in water for injection then sterilizing it.