Abstract:
A method for preparing a 1-[1-(3,4-dialkoxyaryl)-pyridylmethyl]-1H-pyrazole compound is provided to produce a desired product with high purity economically and industrially compared with a method for separating the desired product using a chiral column. A method for preparing a 1-[1-(3,4-dialkoxyaryl)-pyridylmethyl]-1H-pyrazole compound represented by a formula(1) comprises the steps of: (a) subjecting an aryl aldehyde compound represented by a formula(2) and 2-methyl-2-propanesulfinamide to condensation in the presence of titanium ethoxide(Ti(OEt)4) to prepare a compound represented by a formula(4); (b) reacting the compound of the formula(4) with a compound represented by a formula(5) to prepare a compound represented by a formula(6); (c) removing a sulfinyl group of the compound of the formula(6) under acidic condition to prepare an amine compound represented by a formula(7); (d) reacting the compound of the formula(7) with a compound represented by a formula(8) to prepare a cis-type compound represented by a formula(9); and (e) after N-aminating the cis-type compound of the formula(9) by dropping amino 4-nitrobenzoate represented by a formula(10) therein in the existence of a strong base, cyclizing the N-aminated compound to prepare the compound of the formula(1). In the formulae, A is CH; R1 is linear or branched saturated or unsaturated C1-7 alkyl which may be substituted or unsubstituted by halogen; R2 is C3-7 cycloalkyl or (C3-10)cycloalkyl(C1-7)alkyl; and R3 is phenyl which may be substituted by at least one substituent selected from the group consisting of C1-7 alkyl, C3-7 cycloalkyl, (C3-10)cycloalkyl(C1-7)alkyl, C1-7 alkoxy, (C1-7)alkoxy(C1-7)alkyl, (C1-7)alkylsiloxy(C1-7)alkyl, C1-5 alkoxycarbonyl, benzyloxy, halogen, nitro, cyano, C1-7 alkylsiloxy, carboxyl and formyl.
Abstract:
A novel 1,2,4-thiadiazolidine-3,5-dione compound is provided to show excellent activity and enzyme selectivity on Lck SH2, thereby being usefully used for treating and preventing inflammation related diseases such as rheumatoid arthritis with high selectivity without side effects. A pharmaceutical composition for treating and preventing a disease induced by inflammation comprises a 1,2,4-thiadiazolidine-3,5-dione compound represented by a formula(1) or a pharmaceutically acceptable salt thereof as an effective ingredient. In the formula(1), A is linear or branched saturated or unsaturated C1-7 alkyl, indenyl, (C1-7)alkoxycarbonyl(C1-7)alkyl, phenyl, benzyl or C2H5(C=O)HR2R3(wherein A may be substituted by halogen, carboxyl, C1-7 alkoxycarbonyl, C1-7 alkoxy, nitro or hydroxy when A is alkyl, phenyl or benzyl); R1 is H, linear or branched saturated or unsaturated C1-7 alkyl, (C1-7)alkoxycarbonyl(C1-7)alkyl, phenyl, phenyl(C1-5)alkyl or phenylcarbonylmethyl; and each R2 and R2 is independently H, linear or branched saturated or unsaturated C1-7 alkyl or phenyl, or R2 and R3 may form a ring together with C1-5 alkylene. A pharmaceutical composition for treating and preventing rheumatoid arthritis comprises the 1,2,4-thiadiazolidine-3,5-dione compound of the formula(1) or a pharmaceutically acceptable salt thereof as an effective ingredient.
Abstract:
PURPOSE: Provided are derivatives of 9-(5-isoxazolinemethoxyphenyl)imino-8-thia-1.6-diazabicylco£4.3.0|nonane-7-one, represented by the formula(1) and herbicides containing them as active ingredients and having excellent herbicidal activity and selectivity when applied to a rice paddy. CONSTITUTION: Derivatives are represented by the formula(1), wherein R is C1-C6 alkyl, phenyl or substituted phenyl, wherein substituents are 1-3 of halogen atom, C1-C3 alkyl, C1-C3 alkoxy, C1-C3 haloalkyl, cyano, nitro, carboxyl and esters of carboxy acid.
Abstract:
Novel photochromic diarylethenes substituted with an isoxazole group and the method of preparation are disclosed. Also disclosed are compositions made with the photochromic diarylethenes. The preparation of thin films with the photochromic diarylethenes or compositions thereof are disclosed. The photochromic diarylethenes or compositions thereof may be used, for example in recording materials, photochromic windows, indicating elements, plastic mirrors, photochromic filters, photo switches, photosensitive drums, recording elements, solar cells, lens, fibers and optical elements.
Abstract:
PURPOSE: Provided are 5-benzyloxymethyl-1,2-isoxazoline derivatives having an excellent herbicidal activity, its manufacturing method and herbicides containing the derivative as an active ingredient. CONSTITUTION: 5-benzyloxymethyl-1,2-isoxazoline derivative is represented by the formula(I), in which each X1, X2 and X3 represents hydrogen, methyl group, ethyl group, halogen group, methoxy group or nitro group (provided that it is an exception that X1, X2 and X3 are decimals all together); and Y1, Y2 and Y3 are respectively hydrogen or fluorine.
Abstract:
PURPOSE: 2-(5-Isoxazolinyl methyloxyphenyl)-4,5,6,7-tetrahydro-2H-indazole derivatives having herbicidal activity is provided which is useful as herbicides for control of paddy weeds. CONSTITUTION: A herbicidal compound of formula 1, their preparation method and their use as herbicides are described. In formula, X is Cl or hydroxy, R is C1-5 alkyl, substituted or unsubstituted phenyl, cyano, carboxylic acid group, carboxylic acid ester or substituted or unsubstituted hetero. As the compounds have excellent herbicidal activity against paddy weeds comprising ECHOR, SCPJU, MOOVA, CYPSE and SAGPY, and better selectivity, the compounds are typically useful as herbicides for control of paddy weeds in conditions with seeded rice and transferred rice.