Abstract:
본 발명은 3-메칠-(O-치환된 옥시이미노)-피라졸린-5-온 유도체를 함유하는 항암제에 관한 것으로서, 더욱 상세하게는 세포분열에 결정적으로 작용하는 CDC25B의 탈인산화효소에 대한 탁월한 저해활성을 가지고 있는 다음 화학식 1로 표시되는 (O-치환된 옥시이미노)-피라졸린-5-온 유도체가 유효활성 성분으로 함유되어 있는 항암제에 관한 것이다.
상기 화학식 1에서, R 1 및 R 2 는 각각 발명의 상세한 설명에서 정의한 바와 같다.
Abstract:
본 발명은 다음 화학식 1로 표시되는 신규의 9-(5-이속사졸메톡시페닐)이미노-8-치아-1,6-디아자비시클로[4.3.0]노난-7-온 유도체와 이들을 유효성분으로 포함하는 제초제에 관한 것이다.
상기 화학식 1에서, R은 C 1 ∼C 5 의 알킬기, 페닐기 또는 치환된 페닐기이고, 이때 치환된 페닐기는 C 1 ∼C 3 의 알킬기, C 1 ∼C 3 의 알콕시기, 할로겐 원자, 시아노기, 니트로기, 카르복실기 및 카르복실산 에스테르기 중에서 선택된 치환기가 1 ∼ 3개 단일 혹은 복합적으로 치환된 페닐기이다.
Abstract:
PURPOSE: A process for preparing 3-chloro-2- (4-chloro-2-fluoro-5-hydroxyphenyl)- 4,5,6,7-tetrahydro-2H-indazole is provided, thereby improving its preparation yield and converting by-products of the preparation into starting material. CONSTITUTION: A process for preparing 3-chloro-2- (4-chloro-2-fluoro-5-hydroxyphenyl)- 4,5,6,7-tetrahydro-2H-indazole of the formula 1 comprises the steps of: reacting 2- (2-fluoro-4-chloro-5-hydroxyphenyl)- 2,3a,4,5,6,7- hexahydroindazole-3-one of the formula 2 with phosgene; concentrating the phosgene reaction mixture under reduced pressure; dissolving the concentrate in an organic solvent; adding ammonia water or hydroxide solution to the organic solvent and filtering solids; and distilling the filtrated solution, wherein the organic solvent is ethylacetate; the addition of ammonia water or hydroxide solution is carried out at room temperature; the solids are mainly constituted of a compound of the formula 2, and the by-products of the reaction include a dimer represented by the formula 3a, 3b or 3c.
Abstract:
The present invention provided with novel 5-benzyloxymethyl-1,2-isoxazoline derivatives of the formula (1), their preparation method and their use as herbicides. The 5-benzyloxymethyl-1,2-isoxazoline derivatives according to the present invention have sufficiently high herbicidal activity against the weeds in the paddy field rice even at low dose rates and excellent selectivity to transferred rice in particular. As thus, the compounds of the present invention are typically useful as herbicides for control of paddy weeds in rice.
Abstract:
PURPOSE: A N-(5-isoxazolinylmethyloxyphenyl)-dimethylmaleimide derivative is provided which has excellent stability against a rice plant and shows good herbicidal activity on weeds in a paddy like echor, scpju, moova, cypse, sagpy or so on. CONSTITUTION: The N-(5-isoxazolinylmethyloxyphenyl)-dimethylmaleimide derivative is shown in a chemical formula 1 wherein R is alkyl radical with 1-5 carbon number, phenyl radical or substituted phenyl radical, cyano radical, carboxylic acid or carboxylic ester, heterocyclic or substituted heterocyclic radical. The substituted phenyl radical or substituted heterocyclic radical is simply or mixedly substituted from 1-3 radicals among alkyl radical with 1-3 carbon number, alkoxy radial with 1-3 carbon number, halogen atom, cyano radical, nitro radical, carboxyl radical and carboxylic ester.
Abstract:
본 발명은 화학식 1로 표시되는 제초성 3-아릴-테트라히드로-1,2-벤즈이속사졸린-4-온 유도체에 관한 것이다.
상기식에서 Xn은 수소, C 1 -C 4 알킬기, C 2 -C 5 알케닐기, C 2 -C 5 알키닐기, C 1 -C 4 알콕시기, C 1 -C 4 할로알킬기, C 1 -C 4 알콕시카보닐기, 아미노카보닐기, 카복시기, 메탄설포닐기, 니트로기, 히드록시기, 니트릴기, 또는 이들의 둘이상의 복합치환기를 나타낸다.
Abstract:
Title derivatives(I; R1, R2= same or not, H, fluro, chlorro, bromo, C1-3 alkyl, C1-3 alkoxy; R1 and R2 are formed a fused ring such as -CH=CH-CH=CH-; R3= H, C1-4 alkyl, C3-6 alkenyl, etc.), useful as herbicides were prepared. Thus, 3.03 g 4-fluorophenol was reacted with 1.9 ml ethyl chloride, followed by addition of 4.0 g anhydrous aluminium chloride at 180 deg.C for 30 minutes to give 2.71 g 2-hydroxy-5-fluoroacetophenone(III). III and 1.05 g ethyl carbamate were refluxed for 20- 30 hours in 50 ml n-propanol to give ethoxycarbonylhydrazone derivatives IV. 2.41 g IV was dissolved in 100 ml tetrahydrofuran, adding 4.44 g (CH3COO)4Pb as an oxidation agent at room temperature for 3- 5 hours to give ethyl 0-acetylarylcarboxylate derivatives(V). 2.1 g V and 0.83 g 4-chloro-2-fluoro-5-hydroxyaniline were refluxed for 20- 30 hours in a mixed solvent of 50 ml o-dichlorobenzene and acetic acid to give 2,3-dihydro-3-methylene- 2-(4-chloro-2-fluoro-3-hydroxyphenyl)-1H-isoindol-1-one(VII). VII was refluxed for 20 hours to give 2,3-dihydro-3-methylene-2- (3-propagyloxy-4-chloro-2-fluorophenyl)-1H-isoindol-1-one(I).