公开(公告)号：KR1020040014023A

公开(公告)日：2004-02-14

申请号：KR1020020047189

申请日：2002-08-09

Applicant: 한국화학연구원

Inventor： 이규양 ,  이선경 ,  유성은 ,  서지희 ,  김낙정 ,  황선경 ,  김은숙 ,  이병호 ,  서호원 ,  이정옥 ,  최상운

IPC: C07D405/12

CPC classification number: C07D405/12

Abstract: PURPOSE: Benzopyran derivatives substituted by secondary amine containing imidazole and a method for preparing the same are provided. The compounds are useful for treatment of cancer, diabetic retinopathy and external brain wound. CONSTITUTION: Benzopyran derivatives substituted by secondary amine containing imidazole represented by the formula(1), partial stereo isomers thereof and pharmaceutically acceptable salts thereof are provided, wherein R1 is H, CN, NO2 or NH2; R2 is CH3, CHORaRa or CHOOZ; Ra is C1-C4 linear or branched chain alkyl; Z is C2-C6 linear or branched chain alkyl; R3 and R4 are independently H, Cl, Br, F, C1-C3 linear or branched chain alkyl, ORb, CF3, OCF3, NO2 or CO2Rb; Rb is H or C1-C3 alkyl; and * is chiral carbon. A method for preparing the compound of the formula(I) comprises reacting epoxide compounds of the formula(II) with imidazole containing secondary amine compounds of the formula(III) in the presence of metal salt and a solvent, wherein the metal salt is selected from Mg(ClO4)2, COCl2, LiClO4, NaClO4, CaCl2, ZnCl2, LiBF4 and Zn(Tf)2; and the solvent is selected from acetonitrile, tetrahydrofuran and dimethylformamide.

Abstract translation: 目的：提供由含仲胺的咪唑取代的苯并吡喃衍生物及其制备方法。 该化合物可用于治疗癌症，糖尿病性视网膜病变和外部脑部伤口。 构成：提供由式（1）表示的含仲胺的咪唑取代的苯并吡喃衍生物，其部分立体异构体及其药学上可接受的盐，其中R1为H，CN，NO2或NH2; R2是CH3，CHORaRa或CHOOZ; Ra是C1-C4直链或支链烷基; Z是C 2 -C 6直链或支链烷基; R 3和R 4独立地为H，Cl，Br，F，C 1 -C 3直链或支链烷基，ORb，CF 3，OCF 3，NO 2或CO 2 R b; Rb是H或C 1 -C 3烷基; 和*是手性碳。 制备式（I）化合物的方法包括在金属盐和溶剂的存在下使式（II）的环氧化合物与含有式（III）的仲胺化合物的咪唑反应，其中选择金属盐 从Mg（ClO4）2，COCl2，LiClO4，NaClO4，CaCl2，ZnCl2，LiBF4和Zn（Tf）2; 溶剂选自乙腈，四氢呋喃和二甲基甲酰胺。

公开(公告)号：KR100263024B1

公开(公告)日：2000-08-01

申请号：KR1019980013805

申请日：1998-04-17

Applicant: 한국화학연구원

Inventor： 박창식 ,  최은복 ,  김은숙 ,  김병섭

IPC: C07D277/32 ,  A01N43/78 ,  C07D277/42

Abstract: PURPOSE: Provided are novel thiazoleoxyiminoacetamide derivatives represented by the chemical formula I and agricultural/horticultural compositions thereof which have broad spectrum preventive and treatment effect on the plant fungi, especially on rice blast disease (Pyricularia oryzae) and barley powdery mildew (Erysiphe graminis f. sp. hordei). CONSTITUTION: In the chemical formula I, R1 is C1¯C3 alkyl group, phenyl group unsubstituted or substituted with C1¯C3 alkyl/alkoxy or 1¯3 of chloro/fluoro, R4NH or R5CONH where R4 is hydrogen, allyl, or phenyl group unsubstituted or substituted with C1¯C3 alkyl/alkoxy or 1¯3 of chloro/fluoro, R5 is C1¯C3 alkyl, phenyl group unsubstituted or substituted with C1¯C3 alkyl/alkoxy or 1¯3 of chloro/fluoro; R2 is hydrogen, C1¯C3 alkyl, benzyl group, alkyl group substituted with C1¯C3 alkyl thio, alkylsulfonyl; and R3 is C1¯C5 alkyl group.

Abstract translation: 目的：提供由化学式I表示的新型噻唑氧基亚氨基乙酰胺衍生物及其农业/园艺成分，对植物真菌，特别是稻瘟病（Pyricularia oryzae）和大麦白粉病（Erysiphe graminis f。）具有广谱预防和治疗作用。 sp。hordei）。 构成：在化学式I中，R 1为C 1 -C 3烷基，未被取代或被C 1 -C 3烷基/烷氧基取代的苯基或氯/氟，或其中R 4为氢，烯丙基或苯基 未取代或被C 1 -C 3烷基或烷氧基取代或被氯或氟取代，R 5是C 1 -C 3烷基，未被取代或被C 1 -C 3烷基/烷氧基取代的苯基或氯/氟的1-3。 R 2是氢，C 1 -C 3烷基，苄基，被C 1 -C 3烷基硫基取代的烷基，烷基磺酰基; 并且R 3是C 1 -C 5烷基。

公开(公告)号：KR1020000024971A

公开(公告)日：2000-05-06

申请号：KR1019980041817

申请日：1998-10-07

Applicant: 한국화학연구원

Inventor： 박창식 ,  최은복 ,  김은숙 ,  최경자

IPC: C07C251/48

Abstract: PURPOSE: A methoxyacrylate or methoxyimino acetate derivatives, manufacturing method thereof and bactericidal composition using them are provided which have a wide range of antifungal effects against pathogenic bacteria for a variety of plants as well as resistant bacteria and not only a penetrating effect into plants but also a preventing and curing effect on a disease. CONSTITUTION: A methoxyacrylate or methoxyimino acetate derivatives of formula I and amino acid substituted oxime have a wide range of antifungal effects against pathogenic bacteria for a variety of plants as well as resistant bacteria, particularly Pyricularia oryzae, and not only a penetrating effect into plants but also a preventing and curing effect on a disease. The compositions can be also used for pathogenic bacteria for a variety of plants with other components. In formula, R1 is H, C1-C3 alkyl, C1-C3 alkylthio-or alkylsulfon-substituted alkyl, phenyl, or benzyl; R2 is C1-C5 alkyl; X is benzyloxy, C1-C3 alkoxy, C1-C3 alkyl, chloro or fluoro of from 1 to 3, C1-C3 trihaloalkyl, or C1-C3 alkyl or alkoxy-substituted or non substituted phenoxy; Z is CH or N.

Abstract translation: 目的：提供甲氧基丙烯酸酯或甲氧基亚氨基乙酸酯衍生物，其制备方法和使用它们的杀菌组合物，其对各种植物以及抗性细菌具有广泛的针对致病菌的抗真菌作用，并且不仅对植物具有渗透作用 对疾病的预防和治疗效果。 构成：式I的甲氧基丙烯酸酯或甲氧基亚氨基乙酸酯衍生物和氨基酸取代的肟对各种植物以及抗性细菌，特别是Pyricularia oryzae的病原菌具有广泛的抗真菌作用，不仅对植物具有渗透作用， 也是对疾病的预防和治疗效果。 组合物还可用于具有其它成分的各种植物的病原菌。 在式中，R 1是H，C 1 -C 3烷基，C 1 -C 3烷硫基或烷基磺酰基取代的烷基，苯基或苄基; R2是C1-C5烷基; X是1至3的苄氧基，C 1 -C 3烷氧基，C 1 -C 3烷基，氯或氟，C 1 -C 3三卤代烷基或C 1 -C 3烷基或烷氧基取代或未取代的苯氧基; Z是CH或N.

公开(公告)号：KR100492252B1

公开(公告)日：2005-05-30

申请号：KR1020020047189

申请日：2002-08-09

Applicant: 한국화학연구원

Inventor： 이규양 ,  이선경 ,  유성은 ,  서지희 ,  김낙정 ,  황선경 ,  김은숙 ,  이병호 ,  서호원 ,  이정옥 ,  최상운

IPC: C07D405/12

CPC classification number: C07D405/12

Abstract: 본 발명은 이미다졸을 포함하는 이차아민으로 치환된 벤조피란 유도체, 그의 제조방법 및 그를 포함하는 약학적 조성물에 관한 것으로, 본 발명의 벤조피란 유도체는 신생혈관 억제작용, 허혈 심장에 대한 보호작용, 신경세포 보호작용, 지질 과산화 저해작용의 항산화작용을 나타내어 항암제, 류마티스성 관절염 치료제, 당뇨병성 망막증 등의 치료제로 사용될 수 있으며, 심장보호제, 신경세포 보호제, 항산화제 등 산화적 스트레스와 허혈-재관류와 관련된 조직의 보호제 및 질환의 치료제로 사용될 수 있다.

公开(公告)号：KR1020010018591A

公开(公告)日：2001-03-05

申请号：KR1019990034614

申请日：1999-08-20

Applicant: 한국화학연구원

Inventor： 박창식 ,  최은복 ,  김은숙 ,  최경자

IPC: C07D403/14

Abstract: PURPOSE: The 1-phenyl 4-azolyl pyrazole derivatives, a producing method thereof, and a bactericidal composition containing the derivatives useful for agriculture and gardening are provided for killing a wide range of plant bacteria having tolerance to the conventional bactericides. CONSTITUTION: The 1-phenyl 4-azolyl pyrazole derivatives useful as a bactericidal agent are represented by the formula (1), in which n is an integer of 0 to 2; X is 1 to 3 of C1-C3 alkyl, 1 to 3 of chloro, 1 to 3 of fluoro, 1 to 3 of C1-3 alkoxy, nitro, trihaloalkyl, 3,4-ethylenedioxy, or substituted or unsubstituted phenyl or phenoxy; Y is hydrogen, 1 to 3 of C1-C3 alkyl, 1 to 3 of chloro, 1 to 3 of fluoro, 1 to 3 of C1-3 alkoxy, nitro, trihaloalkyl, or substituted or unsubstituted phenyl; and Z is CH or N. The 1-phenyl 4-azolyl pyrazole derivatives is produced by reacting azolyl alpha-oxo ketenedithioacetal of formula (2) with phenylhydrazin of formula (3) in organic solvents. The bactericidal composition contains an effective amount of the 1-phenyl 4-azolyl pyrazole derivatives.

Abstract translation: 目的：提供1-苯基4-噻唑基吡唑衍生物及其制备方法和含有用于农业和园艺的衍生物的杀菌组合物，用于杀死对常规杀菌剂具有耐受性的广泛范围的植物细菌。 构成：用作杀菌剂的1-苯基4-噻唑基吡唑衍生物由式（1）表示，其中n为0-2的整数; X为1至3个C 1 -C 3烷基，1至3个氯，1至3个氟，1至3个C 1-3烷氧基，硝基，三卤代烷基，3,4-亚乙二氧基或取代或未取代的苯基或苯氧基; Y是氢，1至3个C 1 -C 3烷基，1至3个氯，1至3个氟，1至3个C 1-3烷氧基，硝基，三卤代烷基或取代或未取代的苯基; 并且Z是CH或N. 1-苯基4-噻唑基吡唑衍生物通过式（2）的唑基α-氧代烯酮二硫缩醛与式（3）的苯肼在有机溶剂中反应来制备。 该杀菌组合物含有有效量的1-苯基4-唑基吡唑衍生物。

公开(公告)号：KR100373705B1

公开(公告)日：2003-02-25

申请号：KR1019990034614

申请日：1999-08-20

Applicant: 한국화학연구원

Inventor： 박창식 ,  최은복 ,  김은숙 ,  최경자

IPC: C07D403/14

Abstract: PURPOSE: The 1-phenyl 4-azolyl pyrazole derivatives, a producing method thereof, and a bactericidal composition containing the derivatives useful for agriculture and gardening are provided for killing a wide range of plant bacteria having tolerance to the conventional bactericides. CONSTITUTION: The 1-phenyl 4-azolyl pyrazole derivatives useful as a bactericidal agent are represented by the formula (1), in which n is an integer of 0 to 2; X is 1 to 3 of C1-C3 alkyl, 1 to 3 of chloro, 1 to 3 of fluoro, 1 to 3 of C1-3 alkoxy, nitro, trihaloalkyl, 3,4-ethylenedioxy, or substituted or unsubstituted phenyl or phenoxy; Y is hydrogen, 1 to 3 of C1-C3 alkyl, 1 to 3 of chloro, 1 to 3 of fluoro, 1 to 3 of C1-3 alkoxy, nitro, trihaloalkyl, or substituted or unsubstituted phenyl; and Z is CH or N. The 1-phenyl 4-azolyl pyrazole derivatives is produced by reacting azolyl alpha-oxo ketenedithioacetal of formula (2) with phenylhydrazin of formula (3) in organic solvents. The bactericidal composition contains an effective amount of the 1-phenyl 4-azolyl pyrazole derivatives.

Abstract translation: 目的：提供1-苯基-4-唑基吡唑衍生物，其制备方法和含有用于农业和园艺的衍生物的杀菌组合物，用于杀死对常规杀菌剂具有耐受性的各种植物细菌。 构成：可用作杀菌剂的1-苯基4-吡唑基吡唑衍生物由式（1）表示，其中n是0-2的整数; X为C1-C3烷基的1-3个，氯的1-3个，氟的1-3个，C1-3烷氧基的1-3个，硝基，三卤代烷基，3,4-亚乙二氧基或取代或未取代的苯基或苯氧基; Y为氢，C 1 -C 3烷基的1至3个，氯的1至3个，氟的1至3个，C 1-3烷氧基的1至3个，硝基，三卤代烷基或取代的或未取代的苯基; Z是CH或N.1-苯基4-吡唑基吡唑衍生物通过使式（2）的唑基α-氧代酮二硫缩醛与式（3）的苯基肼在有机溶剂中反应来制备。 杀菌组合物含有有效量的1-苯基4-吡唑基吡唑衍生物。

公开(公告)号：KR100383099B1

公开(公告)日：2003-05-12

申请号：KR1020000041639

申请日：2000-07-20

Applicant: 한국화학연구원

Inventor： 박창식 ,  최은복 ,  김은숙 ,  최경자

IPC: C07D403/04

Abstract: PURPOSE: Provided is 3- or 5-amino 4-imidazolyl pyrazole derivatives which has selective bacteriocidal effect on plants. And method of preparing them and an antifungal composition comprising them for agriculture are also provided. CONSTITUTION: 3- or 5-amino 4-imidazolyl pyrazole derivatives are represented by the formula(1), wherein X is hydrogen, chloro group having 1-3 benzene rings, fluoro group having 1-3 benzene rings and C-C3 alkoxy group having 1-3 benzene cycles, nitro group, or phenyl group substituted or unsubstituted trihaloalkyl group; Y is C1-C3 alkyl group; hydrogen; chloro group having 1-3 benzene rings, fluoro group having 1-3 benzene rings, C1-C3 alkoxy group having 1-3 benzene rings, nitro group,or trihaloalkyl group substituted or unsubstituted benzyl group; or chloro group having 1-3 benzene rings, fluoro group having 1-3 benzene rings, C1-C3 alkoxy group having 1-3 benzene rings, nitro group,or trihaloalkyl group substituted or unsubstituted penethyl group; and R is C1-C4 alkyl group; hydrogen; or chloro group having 1-3 benzene rings, fluoro group having 1-3 benzene rings, C1-C3 alkyl group having 1-3 benzene rings, C-C4 alkoxy group having 1-3 benzene rings, nitro group,or trihaloalkyl group substituted or unsubstituted phenyl group.

Abstract translation: 用途：提供对植物具有选择性杀菌效果的3-或5-氨基-4-咪唑基吡唑衍生物。 还提供了它们的制备方法和包含它们的用于农业的抗真菌组合物。 构成：3-或5-氨基-4-咪唑基吡唑衍生物由式（1）表示，其中X是氢，具有1-3个苯环的氯基，具有1-3个苯环的氟基和C 1 -C 3烷氧基 具有1-3个苯环，硝基或苯基取代或未取代的三卤代烷基; Y是C1-C3烷基; 氢; 具有1-3个苯环的氯基，具有1-3个苯环的氟基，具有1-3个苯环的C1-C3烷氧基，硝基或三卤代烷基取代或未取代的苄基; 或具有1-3个苯环的氯基，具有1-3个苯环的氟基，具有1-3个苯环的C1-C3烷氧基，硝基或三卤代烷基取代或未取代的苯甲基; 和R是C1-C4烷基; 氢; 或具有1-3个苯环的氯基，具有1-3个苯环的氟基，具有1-3个苯环的C1-C3烷基，具有1-3个苯环的C-C4烷氧基，硝基或三卤代烷基取代 或未被取代的苯基。

公开(公告)号：KR1020020008242A

公开(公告)日：2002-01-30

申请号：KR1020000041639

申请日：2000-07-20

Applicant: 한국화학연구원

Inventor： 박창식 ,  최은복 ,  김은숙 ,  최경자

IPC: C07D403/04

Abstract: PURPOSE: Provided is 3- or 5-amino 4-imidazolyl pyrazole derivatives which has selective bacteriocidal effect on plants. And method of preparing them and an antifungal composition comprising them for agriculture are also provided. CONSTITUTION: 3- or 5-amino 4-imidazolyl pyrazole derivatives are represented by the formula(1), wherein X is hydrogen, chloro group having 1-3 benzene rings, fluoro group having 1-3 benzene rings and C-C3 alkoxy group having 1-3 benzene cycles, nitro group, or phenyl group substituted or unsubstituted trihaloalkyl group; Y is C1-C3 alkyl group; hydrogen; chloro group having 1-3 benzene rings, fluoro group having 1-3 benzene rings, C1-C3 alkoxy group having 1-3 benzene rings, nitro group,or trihaloalkyl group substituted or unsubstituted benzyl group; or chloro group having 1-3 benzene rings, fluoro group having 1-3 benzene rings, C1-C3 alkoxy group having 1-3 benzene rings, nitro group,or trihaloalkyl group substituted or unsubstituted penethyl group; and R is C1-C4 alkyl group; hydrogen; or chloro group having 1-3 benzene rings, fluoro group having 1-3 benzene rings, C1-C3 alkyl group having 1-3 benzene rings, C-C4 alkoxy group having 1-3 benzene rings, nitro group,or trihaloalkyl group substituted or unsubstituted phenyl group.

Abstract translation: 目的：提供对植物具有选择性杀菌作用的3-或5-氨基-4-咪唑基吡唑衍生物。 还提供了制备它们的方法和包含它们用于农业的抗真菌组合物。 构成：3-或5-氨基-4-咪唑基吡唑衍生物由式（1）表示，其中X是氢，具有1-3个苯环的氯基，具有1-3个苯环的氟基和C-C3烷氧基 具有1-3个苯环，硝基或苯基取代或未取代的三卤代烷基; Y为C1-C3烷基; 氢; 具有1-3个苯环的氯基团，具有1-3个苯环的氟基团，具有1-3个苯环的C1-C3烷氧基，硝基或三卤代烷基取代或未取代的苄基; 或具有1-3个苯环的氯基，具有1-3个苯环的氟基，具有1-3个苯环的C1-C3烷氧基，硝基或三卤代烷基取代或未取代的乙基; 并且R是C 1 -C 4烷基; 氢; 或具有1-3个苯环的氯基，具有1-3个苯环的氟基，具有1-3个苯环的C1-C3烷基，具有1-3个苯环的C-C4烷氧基，硝基或三卤代烷基取代的 或未取代的苯基。

公开(公告)号：KR100270599B1

公开(公告)日：2000-11-01

申请号：KR1019980041817

申请日：1998-10-07

Applicant: 한국화학연구원

Inventor： 박창식 ,  최은복 ,  김은숙 ,  최경자

IPC: C07C251/48

Abstract: 본 발명은 메톡시아크릴레이트 또는 메톡시이미노 아세테이트 유도체, 그의 제조 방법 및 그를 이용한 살균제 조성물에 관한 것이다. 이 유도체 화합물은 하기 화학식 1을 갖고, 아미노산이 치환된 옥심을 갖는다. 이 화합물을 포함하는 살균제 조성물은 내성균을 비롯한 식물 병원균에 대해 광범위한 살균효과를 가지고, 식물에 침투 효과 뿐만 아니라 질병 예방 및 치료 효과가 뛰어나며, 기타 성분과 함께 광범위한 식물 병원균에 대해 사용될 수 있다.
[화학식 1]

상기 식에서,
R
1 는 수소, C
1 -C
3 알킬기, C
1 -C
3 알킬티오- 또는 알킬설폰-치환된 알킬기, 페닐기, 또는 벤질기이고; R
2 은 C
1 -C
5 알킬기이고; X는 벤질옥시, C
1 -C
3 알콕시, C
1 -C
3 알킬기, 1 내지 3개의 클로로 또는 플루오로, C
1 -C
3 트리할로알킬기, 또는 C
1-3 알킬 또는 알콕시-치환되거나 치환되지 않은 페녹시기이고; Z는 CH 또는 N 이다.

公开(公告)号：KR1019990080492A

公开(公告)日：1999-11-15

申请号：KR1019980013805

申请日：1998-04-17

Applicant: 한국화학연구원

Inventor： 박창식 ,  최은복 ,  김은숙 ,  김병섭

IPC: C07D277/32 ,  A01N43/78 ,  C07D277/42

Abstract: 본 발명은 농원예용 살균제로 유용한, 신규한 티아졸옥시이미노아세트아미드 유도체에 관한 것으로, 하기 일반식(I)의 티아졸옥시이미노아세트아미드 유도체는 내성균을 비롯한 식물 병원균에 대해 광범위한 살균효과를 가지고, 침투효과뿐만 아니라 예방 및 치료효과가 뛰어나며, 본 발명의 화합물을 유효성분으로서 유효량 함유하는 살균제 조성물은 기타 성분과 함께 광범위한 식물 병원균에 대해 사용될 수 있다.

상기 식에서,
R
1 은 C
1 -C
3 알킬기, 1 내지 3개의 클로로 또는 플루오로-, 또는 C
1-3 알킬 또는 알콕시-치환되거나 치환되지 않은 페닐기, R
4 NH 또는 R
5 CONH이고(이때, R
4 는 수소, 알릴, 또는 1 내지 3개의 클로로 또는 플루오로-, 또는 C
1-3 알킬 또는 알콕시-치환되거나 치환되지 않은 페닐기이고, R
5 는 C
1 -C
3 알킬기, 또는 1 내지 3개의 클로로 또는 플루오로-, 또는 C
1-3 알킬 또는 알콕시-치환되거나 치환되지 않은 페닐기이다);
R
2 는 수소, C
1 -C
3 알킬기, C
1 -C
3 알킬티오- 또는 알킬설폰-치환된 알킬기, 또는 벤질기이고;
R
3 은 C
1 -C
5 알킬기이다.