公开(公告)号：KR100392074B1

公开(公告)日：2003-08-19

申请号：KR1020000056263

申请日：2000-09-25

Applicant: 한국화학연구원

Inventor： 최일영 ,  이재현 ,  박창식 ,  임희종 ,  김진철

IPC: A01N43/78

Abstract: PURPOSE: A new thiazole derivative obtained by using amide as a starting material is provided which has a strong antibacterial effect on plant pathogenic bacteria with a small amount, for example Pyricularia oryzae Cavera, Rhizoctonia SolaniAG-1, Botrytis cinerea KCI, Phytophthora infestans or the like. CONSTITUTION: Thioamide(formula II) is dissolved in dichloroethane, agitated with dichloroacetone at room temperature for 48 to 72 hr in the presence of a base and then dehydrated to produce chloromethyl thiazole(formula III). A chlorine atom of the chloromethyl thiazole is substituted to an iodine atom by use of sodium iodide and then reacted with 2-(2-hydroxyphenyl)-3-methoxy acrylic acid methylester(formula IV)(in case of A=C) or 2-methoxyimino-(2-hydroxyphenyl)-acetic acid methylester(formula IV)(in case of A=N) to produce a thiazole derivative(formula I).

Abstract translation: 目的：提供一种以酰胺为起始原料得到的新型噻唑衍生物，对植物病原菌有较强的抗菌作用，如Pyricularia oryzae Cavera，Rhizoctonia SolaniAG-1，Botrytis cinerea KCI，致病疫霉或 喜欢。 构成：将硫代酰胺（式II）溶于二氯乙烷中，在室温下用二氯丙酮搅拌48-72小时，然后脱水，生成氯甲基噻唑（式III）。 通过使用碘化钠将氯甲基噻唑的氯原子取代为碘原子，然后与2-（2-羟基苯基）-3-甲氧基丙烯酸甲酯（式IV）（在A = C的情况下）或2 （2-羟基苯基） - 乙酸甲酯（式IV）（在A = N的情况下）反应以产生噻唑衍生物（式I）。

公开(公告)号：KR100217310B1

公开(公告)日：1999-09-01

申请号：KR1019970040068

申请日：1997-08-22

Applicant: 한국화학연구원

Inventor： 이재현 ,  최일영 ,  지성기 ,  박성애 ,  황선애 ,  김병섭

IPC: C07D261/08 ,  C07D413/04

Abstract: 본 발명은 이제까지 살균제로 알려진 바 없는 새로운 구조를 가지며, 각종 식물 병원균에 대해 예방효과를 나타내고, 특히 일부 병원균에 대해 선택적으로 우수한 살균력을 나타내는 다음 화학식 1로 표시되는 신규한 메톡시아크릴레이트 또는 메톡시이미노아세테이트를 함유하는 이속사졸린과 이속사졸 화합물에 관한 것이다.

상기 화학식 1에서, A는 CH 또는 질소원자를 나타내고; X는 페닐기, 치환된 페닐기, 티오펜일기 또는 피리딜기를 나타내며, 이때 치환된 페닐의 치환기로는 할로겐원자, 시아노기, 탄소원자수 1∼3의 알킬기 및 탄소원자수 1∼3의 할로알킬기 중에서 선택된 하나 또는 그 이상의 것이고; Y는 메톡시기로서, 이는 Z- 또는 E-배향을 하며;

公开(公告)号：KR1019960007574A

公开(公告)日：1996-03-22

申请号：KR1019940018975

申请日：1994-08-01

Applicant: 한국화학연구원

Inventor： 이재현 ,  최일영 ,  이수진 ,  김병섭

IPC: C07D413/04 ,  A01N43/72 ,  C07D265/08

Abstract: 본 발명은 식물병원균에 대하여 우수한 살균활성을 갖는 다음 구조식(I)로 표시되는 옥사지닐아졸 유도체와 이를 제조하는 방법에 관한 것이다.

상기 식에서, X는 수소원자, 할로겐원자 또는 트리플르오르메틸기이며, Y는 이미다졸기 또는 트리아졸기이고, R은 C
1 ∼C
4 의 알킬기, 한 개의 할로겐 또는 두 개의 클로로가 치환된 페닐기, 트리플르오르메틸 치환된 페닐기, 2-메틸-4-클로로가 치환된 페닐기 또는 3-메톡시-5-클로로가 치환된 페닐기 등이다.

公开(公告)号：KR100038653B1

公开(公告)日：1990-12-28

申请号：KR1019880006095

申请日：1988-05-24

Applicant: 한국화학연구원

Inventor： 이재현 ,  최일영 ,  김영애 ,  강철훈 ,  김형진 ,  김진석

IPC: C07D309/02

公开(公告)号：KR1020020024487A

公开(公告)日：2002-03-30

申请号：KR1020000056263

申请日：2000-09-25

Applicant: 한국화학연구원

Inventor： 최일영 ,  이재현 ,  박창식 ,  임희종 ,  김진철

IPC: A01N43/78

CPC classification number: A01N43/78 ,  C07D417/04

Abstract: PURPOSE: A new thiazole derivative obtained by using amide as a starting material is provided which has a strong antibacterial effect on plant pathogenic bacteria with a small amount, for example Pyricularia oryzae Cavera, Rhizoctonia SolaniAG-1, Botrytis cinerea KCI, Phytophthora infestans or the like. CONSTITUTION: Thioamide(formula II) is dissolved in dichloroethane, agitated with dichloroacetone at room temperature for 48 to 72 hr in the presence of a base and then dehydrated to produce chloromethyl thiazole(formula III). A chlorine atom of the chloromethyl thiazole is substituted to an iodine atom by use of sodium iodide and then reacted with 2-(2-hydroxyphenyl)-3-methoxy acrylic acid methylester(formula IV)(in case of A=C) or 2-methoxyimino-(2-hydroxyphenyl)-acetic acid methylester(formula IV)(in case of A=N) to produce a thiazole derivative(formula I).

Abstract translation: 目的：提供通过使用酰胺作为起始原料获得的新的噻唑衍生物，其对少量的植物致病菌具有强烈的抗菌作用，例如稻瘟病菌，丝核丝杆菌属（Solricularia oryzae Cavera），丝核菌属（Rhizoctonia SolaniAG-1），灰葡萄孢（Botrytis cinerea KCI），致病疫霉（Phytophthora infestans）或 喜欢。 构成：将硫代酰胺（式II）溶解于二氯乙烷中，在二氯丙酮中在室温下搅拌48-72小时，然后脱水，得到氯甲基噻唑（式Ⅲ）。 氯甲基噻唑的氯原子用碘化钠代替碘原子，然后与2-（2-羟基苯基）-3-甲氧基丙烯酸甲酯（式IV）（在A = C）或2 - 甲氧基亚氨基 - （2-羟基苯基） - 乙酸甲酯（式IV）（在A = N的情况下）以产生噻唑衍生物（式I）。

公开(公告)号：KR100124984B1

公开(公告)日：1997-12-08

申请号：KR1019940018975

申请日：1994-08-01

Applicant: 한국화학연구원

Inventor： 이재현 ,  최일영 ,  이수진 ,  김병섭

IPC: C07D413/04 ,  A01N43/72 ,  C07D265/08

Abstract: Dibromoacetophenone oxime derivatives(III; X= H atom, halogen, trifluoromethyl), useful as fungicides were annulated in the presence of allyl ether base to give bromooxazine derivatives(IV; R= C1-4 alkyl, one halogen or two chloro substituted phenyl, trifluoromethyl substituted phenyl, 2-methyl-4-chloro substituted phenyl or 3-methoxy-5-chloro substituted phenyl), followed by the reaction of imidazole or triazole in the presence of a base to give oxazinylazole derivatives(I; Y= imidazole, triazole). Thus, 10 g of dibromoacetophenone and 6.67 g of hydroxyamine hydrochloride were reacted at room temperature for 4 days in 150 ml of methyl alcohol to give dibromoacetophenone oxime. Obtained 600 mg of oxime was dissolved in 50 ml of anhydrous methylene chloride, followed by adding 750 = allylphenyl ether, and 1.2 g sodium carbonate at room temperature to give 430 mg 3-(4-chlorophenyl)6-phenoxymethyl-5,6-dihydro-4-bromo-1,2-oxazine.

Abstract translation: 可用作杀真菌剂的二溴苯乙酮肟衍生物（III; X = H，卤素，三氟甲基）在烯丙基醚碱存在下进行环化，得到溴恶嗪衍生物（IV; R = C 1-4烷基，一个卤素或二氯取代的苯基， 三氟甲基取代的苯基，2-甲基-4-氯取代的苯基或3-甲氧基-5-氯取代的苯基），然后在碱存在下使咪唑或三唑反应，得到恶唑基衍生物（I; Y =咪唑， 三唑）。 因此，将10g二溴苯乙酮和6.67g羟胺盐酸盐在室温下在150ml甲醇中反应4天，得到二溴苯乙酮肟。 将得到的600mg肟溶于50ml无水二氯甲烷中，然后在室温下加入750 =烯丙基苯基醚和1.2g碳酸钠，得到430mg 3-（4-氯苯基）-6-苯氧基甲基-5,6- 二氢-4-溴-1,2-恶嗪。

公开(公告)号：KR100128575B1

公开(公告)日：1997-11-03

申请号：KR1019940004071

申请日：1994-03-03

Applicant: 한국화학연구원

Inventor： 이재현 ,  김형진 ,  김병섭

IPC: C07D498/04

公开(公告)号：KR100119908B1

公开(公告)日：1997-10-30

申请号：KR1019940008090

申请日：1994-04-18

Applicant: 한국화학연구원

Inventor： 이재현 ,  최일영 ,  김현진 ,  최경자

IPC: C07D405/04

CPC classification number: C07D405/04 ,  A01N43/40

Abstract: Derivatives of 3(2H)-furanone, useful as a bactericidal agent for agriculturee and horticulture are manufactured. Thus, N-oxide compound is added with toluenechloride sufonic acid, heated, and reacted with dimethyl-sufoxide and potassium cyanide at room temperature to give methylcyanopyridine(III), which is reacted with hydroxymethyl aromatic acid ester compound(IV) in the presence of alkali to give aminofuran compound(V). In formula, R is C1-C2 alkyl, propagyl, or 2-chloroallyl, X is halogen, methyl, C1-C2 alkoxy, cyano, thioethyl, or nitro, Y is hologen, methyl, or trifloromethyl.

Abstract translation: 制造用作农业和园艺杀菌剂的3（2H） - 呋喃酮的衍生物。 因此，在室温下加入N-甲氧基化合物，加热并与二甲基 - 氧化亚锡和氰化钾反应，得到甲基氰基吡啶（III），其与羟甲基芳族酸酯化合物（IV）在存在 得到氨基呋喃化合物（Ⅴ）。 在式中，R是C 1 -C 2烷基，扩链或2-氯烯丙基，X是卤素，甲基，C 1 -C 2烷氧基，氰基，硫代乙基或硝基，Y是氢原子，甲基或三氟甲基。

公开(公告)号：KR1019970011394B1

公开(公告)日：1997-07-10

申请号：KR1019940004071

申请日：1994-03-03

Applicant: 한국화학연구원

Inventor： 이재현 ,  김형진 ,  김병섭

IPC: C07D498/04

Abstract: Halo alcohol compound is halogenated by trihalophosphate in diethylether as solvent to yield dihalogented compound, thereafter, yielded compound is reacted with amines of R2-NH2 in the presence of base such as sodium carbonate and potassium carbonate in organic solvent such as ethanol, dimethyl formamide and dimethyl sulfoxide to yield compound represented by general formula(I). In general formula(I), R1 represents phenyl group or halogen atoms, R2 represents alkyl group having 1 to 5 of carbon atoms.

Abstract translation: 卤代醇化合物被三乙酸酯在乙醚中作为溶剂卤化，得到二卤化合物，然后在有机溶剂如乙醇，二甲基甲酰胺等有机溶剂如碳酸钠和碳酸钾存在下，使得到的化合物与R2-NH2的胺反应， 二甲基亚砜，得到通式（I）表示的化合物。 通式（I）中，R 1表示苯基或卤原子，R 2表示碳原子数1〜5的烷基。

公开(公告)号：KR1019950029263A

公开(公告)日：1995-11-22

申请号：KR1019940008090

申请日：1994-04-18

Applicant: 한국화학연구원

Inventor： 이재현 ,  최일영 ,  김현진 ,  최경자

IPC: C07D405/04

Abstract: 본 발명은 식물병원균에 대하여 우수한 살균활성을 갖는다는 다음 구조식(Ⅰ)로 표시되는 신규한 3(2H)―푸란온 유도체 및 이를 제조하는 방법에 관한 것이다.

상기식에서, R은 C
1 ∼C
2 의 알킬, 프로파길 또는 2―클로로알릴기이고, X는 할로겐원자, 메틸, C
1 ∼C
2 의 알콕시, 시아노, 티오에틸 또는 니트로기이며, Y는 할로겐원자, 메틸 또는 트리플로로메틸기이다.