1-[1-(3,4-디알콕시아릴)-피리딜메틸]-1H-피라졸 화합물의제조방법
    101.
    发明授权
    1-[1-(3,4-디알콕시아릴)-피리딜메틸]-1H-피라졸 화합물의제조방법 失效
    制备1- [1-(3,4-二氮代烷基) - 吡咯烷基] -1H-吡唑化合物的方法

    公开(公告)号:KR100838702B1

    公开(公告)日:2008-06-16

    申请号:KR1020070013408

    申请日:2007-02-08

    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 translation: 提供了一种制备1- [1-(3,4-二烷氧基芳基) - 吡啶基甲基] -1H-吡唑化合物的方法,与使用手性的分离所需产物的方法相比,在经济和工业上产生具有高纯度的所需产物 柱。 制备由式(1)表示的1- [1-(3,4-二烷氧基芳基) - 吡啶基甲基] -1H-吡唑化合物的方法包括以下步骤:(a)使由式 2)和2-甲基-2-丙磺酰胺在乙醇钛(Ti(OEt)4)存在下缩合以制备由式(4)表示的化合物; (b)使式(4)的化合物与式(5)表示的化合物反应,制备由式(6)表示的化合物; (c)在酸性条件下除去式(6)化合物的亚磺酰基以制备由式(7)表示的胺化合物; (d)使式(7)的化合物与式(8)表示的化合物反应,制备由式(9)表示的顺式化合物; 和(e)通过在存在强碱的情况下滴加由式(10)表示的式(10)表示的氨基-4-硝基苯甲酸将式(9)的顺式式化合物N-胺化后,使N-胺化化合物环化以制备 式(1)的化合物。 在式中,A为CH; R1是可被卤素取代或未取代的直链或支链饱和或不饱和C 1-7烷基; R2是C3-7环烷基或(C3-10)环烷基(C1-7)烷基; 并且R 3是可以被至少一个选自C 1-7烷基,C 3-7环烷基,(C 3-10)环烷基(C 1-7)烷基,C 1-7烷氧基, 7)烷氧基(C 1-7)烷基,(C 1-7)烷基甲硅烷氧基(C 1-7)烷基,C 1-5烷氧基羰基,苄氧基,卤素,硝基,氰基,C 1-7烷基甲硅烷氧基,羧基和甲酰基。

    1,2,4-티아다이아졸리딘-3,5-다이온 화합물을 포함하는염증관련 질환의 치료 및 예방을 위한 약제학적 조성물
    102.
    发明授权
    1,2,4-티아다이아졸리딘-3,5-다이온 화합물을 포함하는염증관련 질환의 치료 및 예방을 위한 약제학적 조성물 失效
    用于治疗或预防包含1,2,4-噻二唑-3,5-二酮化合物的药物的药物组合物

    公开(公告)号:KR100837785B1

    公开(公告)日:2008-06-13

    申请号:KR1020070005148

    申请日:2007-01-17

    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 translation: 提供了一种新的1,2,4-噻二唑烷-3,5-二酮化合物,以显示对Lck SH2的极好的活性和酶选择性,从而有效地用于治疗和预防炎症相关疾病如类风湿性关节炎,具有高选择性,无副作用 。 用于治疗和预防炎性疾病的药物组合物包含由式(1)表示的1,2,4-噻二唑烷-3,5-二酮化合物或其药学上可接受的盐作为有效成分。 在式(1)中,A是直链或支链饱和或不饱和的C1-7烷基,茚基,(C1-7)烷氧基羰基(C1-7)烷基,苯基,苄基或C2H5(C = O)HR2R3(其中A可以 苯基或苄基)被卤素,羧基,C 1-7烷氧基羰基,C 1-7烷氧基,硝基或羟基取代。 R1是H,直链或支链饱和或不饱和的C1-7烷基,(C1-7)烷氧基羰基(C1-7)烷基,苯基,苯基(C1-5)烷基或苯基羰基甲基; 并且每个R 2和R 2独立地为H,直链或支链饱和或不饱和的C 1-7烷基或苯基,或者R 2和R 3可与C 1-5亚烷基一起形成环。 用于治疗和预防类风湿性关节炎的药物组合物包含式(1)的1,2,4-噻二唑烷-3,5-二酮化合物或其药学上可接受的盐作为有效成分。

    제초활성을 갖는9-(5-이속사졸린메톡시페닐)이미노-8-치아-1,6-디아자비시클로[4.3.0]노난-7-온 유도체
    103.
    发明授权
    제초활성을 갖는9-(5-이속사졸린메톡시페닐)이미노-8-치아-1,6-디아자비시클로[4.3.0]노난-7-온 유도체 失效
    제초활성을갖는9-(5-이속사졸린메톡시페닐)이미노-8-치아-1,6디아자비시클로[4.3.0]노난-7-온유도체

    公开(公告)号:KR100454099B1

    公开(公告)日:2004-10-26

    申请号:KR1020020049819

    申请日:2002-08-22

    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 translation: 用途:提供由式(1)表示的9-(5-异恶唑啉甲氧基苯基)亚氨基-8-硫杂-1,6-二氮杂双环[4.3.0]壬烷-7-酮的衍生物和含有它们作为活性成分的除草剂, 除草活性和选择性,当应用到稻田。 构成:衍生物由式(1)表示,其中R为C 1 -C 6烷基,苯基或取代的苯基,其中取代基为卤素原子,C 1 -C 3烷基,C 1 -C 3烷氧基,C 1 -C 3卤代烷基, 氰基,硝基,羧基和羧酸的酯。

    이속사졸기로 치환된 신규한 광변색성 디아릴에텐계 화합물
    104.
    发明授权

    公开(公告)号:KR100424862B1

    公开(公告)日:2004-03-31

    申请号:KR1020010011544

    申请日:2001-03-06

    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 translation: 公开了用异恶唑基团取代的新型光致变色二芳基乙烯化合物和制备方法。 还公开了用光致变色二芳基乙烯制成的组合物。 公开了用光致变色二芳基乙烯或其组合物制备薄膜。 光致变色二芳基乙烯或其组合物可用于例如记录材料,光致变色窗,指示元件,塑料镜,光致变色滤光片,光敏开关,感光鼓,记录元件,太阳能电池,透镜,纤维和光学元件。

    제초활성을 갖는 5-벤질옥시메틸-1,2-이속사졸린 유도체화합물
    105.
    发明公开
    제초활성을 갖는 5-벤질옥시메틸-1,2-이속사졸린 유도체화합물 有权
    具有除草活性的5-苄氧基甲基-1,6-异恶唑烷酮衍生物

    公开(公告)号:KR1020020019751A

    公开(公告)日:2002-03-13

    申请号:KR1020000052918

    申请日:2000-09-07

    CPC classification number: A01N43/80 C07D413/04

    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 translation: 目的:提供具有优异除草活性的5-苄氧基甲基-1,2-异恶唑啉衍生物,其制造方法和含有该衍生物作为活性成分的除草剂。 构成:5-苄氧基甲基-1,2-异恶唑啉衍生物由式(I)表示,其中X1,X2和X3各自表示氢,甲基,乙基,卤素基,甲氧基或硝基(条件是它 是一个例外,X1,X2和X3都是小数) Y1,Y2和Y3分别为氢或氟。

    제초활성을 가지는 2-(5-이속사졸린메틸옥시페닐)-4,5,6,7-테트라히드로-2H-인다졸 유도체
    107.
    发明公开
    제초활성을 가지는 2-(5-이속사졸린메틸옥시페닐)-4,5,6,7-테트라히드로-2H-인다졸 유도체 失效
    除草剂2-(5-异丙唑基甲氧基苯基)-4,5,6,7-四氢-2H-吲哚衍生物

    公开(公告)号:KR1020000056677A

    公开(公告)日:2000-09-15

    申请号:KR1019990006209

    申请日:1999-02-25

    CPC classification number: C07D413/12 A01N43/80

    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.

    Abstract translation: 目的:提供具有除草活性的2-(5-异唑啉基甲氧基苯基)-4,5,6,7-四氢-2H-吲唑衍生物,其可用作防治稻田杂草的除草剂。 构成:描述了式1的除草化合物,其制备方法及其作为除草剂的用途。 在式中,X为Cl或羟基,R为C 1-5烷基,取代或未取代的苯基,氰基,羧酸基,羧酸酯或取代或未取代的杂原子。 由于化合物对包括ECHOR,SCPJU,MOOVA,CYPSE和SAGPY的稻田杂草具有优异的除草活性,并且具有更好的选择性,所以化合物通常可用作用于在播种稻和转移稻的条件下控制稻田杂草的除草剂。

Patent Agency Ranking