-
公开(公告)号：KR100460449B1
公开(公告)日：2004-12-08
申请号：KR1020010072183
申请日：2001-11-20
Applicant: 한국화학연구원
IPC: C07C69/743
Abstract: PURPOSE: A method for preparing bifenthrin is provided, to obtain bifenthrin with the improved production yield under the milder condition by employing the thioacyl dithiophosphate as an intermediate. CONSTITUTION: The method comprises the steps of reacting the 3-(2-chloro-3,3,3-trifluoro-1-propenyl)-2,2-dimethyl cyclopentane carboxylic acid alkyl ester represented by the formula 2 with the dithiophosphate represented by the formula 3 to prepare the thioacyl dithiophosphate represented by the formula 4; and reacting the thioacyl dithiophosphate of the formula 4 with the 2-methyl-biphenyl-3-yl-methanol represented by the formula 5 to prepare the bifenthrin represented by the formula 1, wherein R1 and R2 are an alkyl group of C1-C6, respectively. Preferably the first step is carried out with stirring the mixture in the presence of an amine base; and the second step is carried out in the presence of an amine base at a room temperature.
Abstract translation: 目的：提供一种制备联苯菊酯的方法，通过使用硫代酰基二硫代磷酸酯作为中间体，在较温和的条件下获得具有提高的产量的联苯菊酯。 构成：该方法包括使由式2表示的3-（2-氯-3,3,3-三氟-1-丙烯基）-2,2-二甲基环戊烷羧酸烷基酯与由式2表示的二硫代磷酸酯 用于制备由式4表示的硫代酰基二硫代磷酸酯的式3; 并使式4的硫代酰基二硫代磷酸酯与式5代表的2-甲基 - 联苯-3-基 - 甲醇反应，以制备式1代表的联苯菊酯，其中R1和R2为C1-C6烷基， 分别。 优选地，第一步骤是在胺碱存在下搅拌混合物进行的; 第二步在室温下在胺碱存在下进行。
-
公开(公告)号：KR1020030041410A
公开(公告)日：2003-05-27
申请号：KR1020010072183
申请日：2001-11-20
Applicant: 한국화학연구원
IPC: C07C69/743
Abstract: PURPOSE: A method for preparing bifenthrin is provided, to obtain bifenthrin with the improved production yield under the milder condition by employing the thioacyl dithiophosphate as an intermediate. CONSTITUTION: The method comprises the steps of reacting the 3-(2-chloro-3,3,3-trifluoro-1-propenyl)-2,2-dimethyl cyclopentane carboxylic acid alkyl ester represented by the formula 2 with the dithiophosphate represented by the formula 3 to prepare the thioacyl dithiophosphate represented by the formula 4; and reacting the thioacyl dithiophosphate of the formula 4 with the 2-methyl-biphenyl-3-yl-methanol represented by the formula 5 to prepare the bifenthrin represented by the formula 1, wherein R1 and R2 are an alkyl group of C1-C6, respectively. Preferably the first step is carried out with stirring the mixture in the presence of an amine base; and the second step is carried out in the presence of an amine base at a room temperature.
Abstract translation: 目的：提供一种用于制备联苯菊酯的方法，通过使用硫代酰基二硫代磷酸酯作为中间体，在较温和的条件下获得具有改善的产率的联苯菊酯。 构成：该方法包括使由式2表示的3-（2-氯-3,3,3-三氟-1-丙烯基）-2,2-二甲基环戊烷羧酸烷基酯与由式2表示的二硫代磷酸酯 式3制备由式4表示的硫代酰基二硫代磷酸酯; 并使式4的硫代酰基二硫代磷酸酯与式5表示的2-甲基 - 联苯-3-基 - 甲醇反应，制备由式1表示的联苯菊酯，其中R1和R2是C1-C6烷基， 分别。 优选地，在胺基存在下搅拌混合物进行第一步骤; 第二步是在室温下在胺碱的存在下进行。
-
公开(公告)号：KR1020040100302A
公开(公告)日：2004-12-02
申请号：KR1020030032597
申请日：2003-05-22
IPC: C07F9/08
CPC classification number: C07F9/09
Abstract: PURPOSE: A process for preparing bomyl derivatives is provided, which process reduces the number of reaction processes and inhibits release of harmful gas, and which bomyl derivatives have improved insecticidal activity. CONSTITUTION: The process for preparing bomyl derivatives represented by formula (1) comprises reacting tri-keto ester of formula (2) with chloro phosphate of formula (3) in the presence of base at -76 to 0 deg. C for 1 to 5 hours, wherein R1 and R2 are independently C1-C5 lower alkyl group; the base is selected from triethylamine, trimethylamine, diisopropylamine, N-methylmorpholine and DBU(1,8-diazabicyclo(5,4,0)undes-7-ene); and the reaction solvent is dichloromethane, chloroform or dichloroethane.
Abstract translation: 目的：提供一种制备溴代衍生物的方法，该方法减少了反应过程的数量，抑制了有害气体的释放，而且哪些苯甲酰衍生物具有改善的杀虫活性。 构成：由式（1）表示的制备苯甲酰基衍生物的方法包括在碱存在下在-76至0℃下使式（2）的三酮酯与式（3）的氯磷酸酯反应。 C 1〜5小时，其中R 1和R 2独立地为C 1 -C 5低级烷基; 碱选自三乙胺，三甲胺，二异丙胺，N-甲基吗啉和DBU（1,8-二氮杂双环（5,4,0）不饱和7-烯）; 反应溶剂为二氯甲烷，氯仿或二氯乙烷。
-
Patent Agency Ranking
公开(公告)号：KR100726672B1
公开(公告)日：2007-06-11
申请号：KR1020030027709
申请日：2003-04-30
Applicant: 한국화학연구원
IPC: C07D403/04
Abstract: 본 발명은 피라졸 유도체 및 그의 제조방법에 관한 것으로, 본 발명에 따라, 하기 화학식 1의 화합물을 알칼리 염기 존재 하에서 여러가지 친핵체와 친핵 치환 반응시켜 하기 화학식 2의 다양한 피라졸 유도체를 온화한 조건하에서 제조할 수 있으며, 본 발명에 따라 제조된 신규한 피라졸 유도체들은 신약개발을 위한 신규물질이나, COX-2 억제제, 항생제, 살충제 등 여러 가지 생물학적 효능을 지닌 화합물 합성의 중간체로서 유용하게 사용될 수 있다.
상기 식에서,
R
1 은 수소, C
1 -C
5 저급 알킬, C
1 -C
5 저급 할로알킬, 아릴, 아미노, 알킬아미노, 하이드록시 또는 할로겐이고,
R
2 는 수소, C
1 -C
5 저급 알킬, C
1 -C
5 저급 할로알킬, 아릴, 피리딘, 아미노, 알킬아미노 또는 할로겐이고,
X는 할로겐이며,
Nu는 수소; 피롤, 피라졸, 이미다졸, 피페라진, 모폴린, 피롤리딘과 같은 복소환; 아릴; 하이드록시; 아미노; 알킬아미노 또는 할로겐이다.-
公开(公告)号：KR100525468B1
公开(公告)日：2005-11-02
申请号：KR1020020073763
申请日：2002-11-26
Applicant: 한국화학연구원
IPC: C07D231/20
Abstract: 본 발명은 펜프록시메이트(fenpyroximate)의 개선된 제조방법에 관한 것으로, 알칼리 염기 존재하에 5-할로-1,3-디메틸-1
H -피라졸-4-카브알데히드를 페놀과 가열반응시켜 반응중간체로 사용되는 1,3-디메틸-5-페녹시-1
H -피라졸-4-카브알데히드를 제조하거나; 또는 산 존재하에 4-할로메틸벤조산을 t-부탄올과 반응시켜 반응중간체로 사용되는 4-할로메틸벤조산 t-부틸에스테르를 제조하는 것을 특징으로 하며, 이러한 본 발명의 개선된 중간체 제법에 의하면, 최종 목적화합물인 하기 화학식 1의 펜프록시메이트를 기존의 방법에 비해 보다 온화한 조건하에서 고수율로 제조할 수 있다.-
公开(公告)号：KR1020040093857A
公开(公告)日：2004-11-09
申请号：KR1020030027709
申请日：2003-04-30
Applicant: 한국화학연구원
IPC: C07D403/04
Abstract: PURPOSE: A pyrazole derivative and a preparation method thereof are provided, thereby preparing the pyrazole derivative having antimicrobial and insecticidal activity under mild condition. CONSTITUTION: The pyrazole derivative is represented by the formula (2), wherein R1 is hydrogen, C1-C5 lower alkyl, C1-C5 lower haloalkyl, aryl, amino, alkylamino, hydroxy or halogen atom; R2 is hydrogen, C1-C5 lower alkyl, C1-C5 lower haloalkyl, aryl, pyridinyl, amino, alkylamino or halogen atom; and Nu is hydrogen, heterocyclic compound such as pyrrole, pyrazol, imidazol, piperazine, morpholine and pyrrolidine, aryl, hydroxy, amino, alkylamino or halogen atom. The method for preparing the pyrazole derivative of the formula (2) comprises nucleus substitution of a compound of the formula (1) with a nucleophilic substituent of the formula (3) in an organic solvent in the presence of base, wherein X is halogen, and Y is hydrogen or alkali metal such as sodium and potassium.
Abstract translation: 目的：提供吡唑衍生物及其制备方法，从而制备在温和条件下具有抗微生物和杀虫活性的吡唑衍生物。 构成：吡唑衍生物由式（2）表示，其中R 1是氢，C 1 -C 5低级烷基，C 1 -C 5低级卤代烷基，芳基，氨基，烷基氨基，羟基或卤素原子; R2是氢，C1-C5低级烷基，C1-C5低级卤代烷基，芳基，吡啶基，氨基，烷基氨基或卤素原子; 并且Nu是氢，杂环化合物如吡咯，吡唑，咪唑，哌嗪，吗啉和吡咯烷，芳基，羟基，氨基，烷基氨基或卤素原子。 制备式（2）的吡唑衍生物的方法包括式（1）化合物与式（3）的亲核取代基在有机溶剂中在碱存在下的核取代，其中X是卤素， Y是氢或碱金属如钠和钾。
-
公开(公告)号：KR1020040045982A
公开(公告)日：2004-06-05
申请号：KR1020020073763
申请日：2002-11-26
Applicant: 한국화학연구원
IPC: C07D231/20
Abstract: PURPOSE: An improved process for preparing fenpyroximate is provided, thereby preparing fenpyroximate in higher yield under mild condition by improving the preparation process of pyrazol derivatives and benzoic acid t-butylester derivatives. CONSTITUTION: The improved process for preparing fenpyroximate represented by formula 1 comprises the steps of: (a) heat reacting a compound of formula 4 with a compound of formula 5 in organic solvent in the presence of alkali base to prepare a compound of formula 2; and (b) reacting the compound of formula 2 with a compound of formula 10 in inactive solvent, or reacting the compound of formula 2 with a compound of formula 8: H2NO-Z in organic solvent to prepare a compound of formula 9 and reacting the compound of formula 9 with a compound of formula 3 in inactive solvent, wherein X is halogen atom; the alkali base is sodium hydroxide, potassium hydroxide, lithium hydroxide, sodium carbonate, sodium bicarbonate or cesium carbonate; and the reaction temperature is 110 to 130 deg. C.
Abstract translation: 目的：提供一种改进的制备新戊酰亚胺的方法，从而通过改进吡唑衍生物和苯甲酸叔丁酯衍生物的制备方法，在温和条件下以更高的产率制备茴香酸。 构成：由式1制备新戊酸的改进方法包括以下步骤：（a）在碱存在下，在有机溶剂中使式4化合物与式5化合物反应，制备式2化合物; 和（b）使式2的化合物与式10的化合物在惰性溶剂中反应，或使式2化合物与式8化合物：H 2 NO-Z在有机溶剂中反应，以制备式9的化合物，并使 式9的化合物与式3的化合物在无活性溶剂中，其中X是卤素原子; 碱性碱为氢氧化钠，氢氧化钾，氢氧化锂，碳酸钠，碳酸氢钠或碳酸铯; 反应温度为110〜130℃。 C。
-
公开(公告)号：KR100563581B1
公开(公告)日：2006-03-27
申请号：KR1020030032597
申请日：2003-05-22
IPC: C07F9/08
Abstract: 본 발명은 하기 화학식 1로 표시되는 보밀(bomyl) 유도체의 개선된 제조방법에 관한 것으로, 특히 트리-케토 에스테르에 염기와 클로로포스페이트와 같은 친전자체를 사용하여 친전자체를 선택적으로 산소원자에 부가하는 엔올(enol) 합성반응을 통해 보다 간편하고 온화한 반응조건에서 한 번에 반응을 완료할 수 있는 보밀 유도체의 제조 방법에 관한 것이다.
상기 식에서, R
1 및 R
2 는 각각 독립적으로 C
1 ∼ C
5 의 저급 알킬기이다.
-
-
-
-
-
-
-
Search Results
8
records
(took 0.019 seconds)
