Abstract:
PURPOSE: A pharmaceutical composition containing triazole compounds for treating tuberculosis is provided to be used as an anti-tuberculosis therapeutic agent. CONSTITUTION: A triazole compound is denoted by chemical formula 1 or 2. In chemical formula 1 or 2, R1 is aryl or heteroaryl; R2 is hydroxy, keto, amino, azido, C1-16 alkyl amino, and C1-6 acyl amino group. A pharmaceutical composition for treating tuberculosis contains a triazole compound of chemical formula 1a or pharmaceutically acceptable salt thereof as an active ingredient.
Abstract:
A method for preparing a beta-azido carbonyl compound is provided to obtain an intermediate useful for preparing beta-amino acids or aminoalcohols used in various medicines, particularly in beta-lactam antibiotics, HIV-protease inhibitor, etc., by a simple process with high efficiency. The method for preparing a beta-azido carbonyl compound represented by a formula 1 comprises a step of reacting an alpha, beta-unsaturated compound represented by a formula 2 with sodium azide in an organic solvent in the presence of hydrochloric acid and an organic catalyst. In the formulae 1 and 2, R1 is H or a C1-C6 alkyl; and R2 is H, a C1-C10 alkyl or hydroxy methyl substituted with benzyloxy, methyoxy or benzoyloxy, allyl group, or ester group.
Abstract:
본 발명은 2-아미노피리딘 유도체를 제조하는 방법에 관한 것으로, 본 발명에 따라 3-치환-2,5,6-트리플루오르피리딘을 히드라진 일수화물과 반응시켜 히드라지노기를 도입시킨 후, 바로 수소로 환원반응 시키거나, 또는 히드라지노기를 탈리시킴으로써 불소 치환기 하나를 제거하고 다시 히드라진 일수화물과 반응시켜 히드라지노기를 도입시켜 수소로 환원반응 시키는 단계를 포함하는 2-아미노-3-플루오르피리딘 유도체를 제조하는 방법은, 저가의 원료물질들을 사용하여 산업적 적용이 용이한 공정을 통해 2-아미노피리딘 유도체를 고순도로 제조할 수 있으므로, CCR(cellular chemokine receptor: 세포화학수용체)5 모듈레이터(modulator)의 제조 뿐만 아니라 감염증 치료제(anti-infective agents)의 제조 등에 유용하게 활용될 수 있다.
Abstract:
PURPOSE: Provided is a preparation method of secondary amide in high purity and yield from tertiary amide by elimination of β-substituted α-arylalkyl group in reaction with protonic acid in organic solvent. The α-arylethylamine or α-aryl-β-substituted ethylamine is used as a nitrogen source in synthesis of biologically active compounds. CONSTITUTION: The synthesis of the secondary amide is characterized by making a tertiary amide represented by the formula(2) react with protonic acid in organic solvent to manufacture a secondary amine represented by the formula(1) by stirring at 10-150 deg.C for 2-24 hours. In the formulae, R1 is C1-5 alkyl, C3-7cycloalkyl, heterocyclic or C6-15 aryl group substituted with one or more groups selected from low alkyl with C1-4, hydroxy, animo, halogen, alkoxy, monoalkylamino, dialkylamino and carboxyl group; R2 is C1-5 alkyl group substituted with more than one group selected from amino, hydroxy, mono alkylamino, alkoxy and halogen; Ar is phenyl or α- or β-naphthyl group substituted by one or more groups selected from halogen, methoxy, carbamoyl, sulfamoyl, nitro group; R3 is C6-15 alkyl, phenyl or heterocyclic group substituted by one or more groups selected from C1-4 low alkyl, hydroxy, amino, halogen, alkoxy, mon alkylamino, dialkyl amino, carboxyl, carbamoyl, sulfamoyl, nitro or cyano group; and R1 and R3 are connected to form a 5 or 6 membered ring. The protonic acid is selected from hydrochloric acid, acetic acid, trifluoroacetic acid and methanesulfonic acid.
Abstract:
PURPOSE: Provided is a preparation method of secondary amide in high purity and yield from tertiary amide by elimination of β-substituted α-arylalkyl group in reaction with protonic acid in organic solvent. The α-arylethylamine or α-aryl-β-substituted ethylamine is used as a nitrogen source in synthesis of biologically active compounds. CONSTITUTION: The synthesis of the secondary amide is characterized by making a tertiary amide represented by the formula(2) react with protonic acid in organic solvent to manufacture a secondary amine represented by the formula(1) by stirring at 10-150 deg.C for 2-24 hours. In the formulae, R1 is C1-5 alkyl, C3-7cycloalkyl, heterocyclic or C6-15 aryl group substituted with one or more groups selected from low alkyl with C1-4, hydroxy, animo, halogen, alkoxy, monoalkylamino, dialkylamino and carboxyl group; R2 is C1-5 alkyl group substituted with more than one group selected from amino, hydroxy, mono alkylamino, alkoxy and halogen; Ar is phenyl or α- or β-naphthyl group substituted by one or more groups selected from halogen, methoxy, carbamoyl, sulfamoyl, nitro group; R3 is C6-15 alkyl, phenyl or heterocyclic group substituted by one or more groups selected from C1-4 low alkyl, hydroxy, amino, halogen, alkoxy, mon alkylamino, dialkyl amino, carboxyl, carbamoyl, sulfamoyl, nitro or cyano group; and R1 and R3 are connected to form a 5 or 6 membered ring. The protonic acid is selected from hydrochloric acid, acetic acid, trifluoroacetic acid and methanesulfonic acid.
Abstract:
PURPOSE: A preparation method of 1,3,5-substituted 2,4,6-triiodobenzene derivatives by reacting 1,3,5-substituted benzene derivatives with iodine chloride(ICI) and a base is provided which gives a high-purity product in a high yield. CONSTITUTION: 2,4,6-Triiodobenzene derivatives(1) substituted in the 1,3,5-position are prepared by reacting 1,3,5-substituted benzene derivatives(2) with iodine chloride(ICI) and a base in a mixture solvent of methanol and dichloromethane(CH2Cl2) at 0-80°C for 0.5-60 hr. In formula, R1 is a hydroxy, amino or nitro group; R2, R3 are independently 1-5C alkyl, CO2R4 or COR5; R4 is H or C1-7 alkyl; R5 is 1-3C alkyl amino, -N(R6)CH2CH(OR7)CH2OR7, -N(R6)CH(CH2OR7)CH(OR7)CH(OR7)CH2OR7 or -N(R6)CH(CH2OR7)CHOR7(R6,R7 are independently H, 1-2C alkyl or 1-3C acyl). The mixture ratio of methanol to dichloromethane is 1: 1 - 10: 1. The product is useful as an important intermediate of a contrast medium of X-rays.
Abstract:
하기 화학식 1의 4-옥소-퀴놀리진-3-카르복실산 유도체, 그의 라세미 화합물, 거울상 이성질체 또는 입체 이성질체, 및 그의 제약학적으로 허용되는 염이 제공된다.
식 중, R 1 은 탄소 원자수 1 내지 4의 저급 알킬기, 할로겐으로 치환된 탄소 원자수 1 내지 4의 저급 알킬기 또는 탄소 원자수 1 내지 4의 저급 알콕시기이고, R 2 는 고리형 아민이고, R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , R 11 , R 12 , R 13 및 R 14 는 서로 동일하거나 또는 상이한 것으로서, 각각 H, 탄소 원자수 1 내지 4의 저급 알킬기, 또는 피리딜 또는 아릴로 치환된 탄소 원자수 1 내지 4의 저급 알킬기이다.
Abstract:
본 발명은 하기 일반식(I)의 신규한 퀴놀론카르복실산 유도체 및 그의 약제학적으로 허용되는 염, 그의 제조방법 및 이를 활성 성분으로 함유하는 항균 조성물에 관한 것으로, 일반식(I)의 화합물은 항균력이 우수하고, 광범위한 항균 스펙트럼을 가지므로 항균제로 유용하다.
(상기식에서, X, R 1 , R 2 , R 3 , R 4 , R 5 및 R 6 은명세서중에서 정의한 바와 같다).