公开(公告)号：KR100510430B1

公开(公告)日：2005-08-26

申请号：KR1020020038011

申请日：2002-07-02

Applicant: 제노마인(주) ,  한국화학연구원

Inventor： 이동희 ,  고재흥 ,  김태훈 ,  박유신 ,  조광연 ,  황인택 ,  최정섭 ,  민용기 ,  김태준 ,  이선우

IPC: C12N9/10

CPC classification number: C12N9/1029 ,  C12N15/8261 ,  C12N15/8263 ,  C12N15/8274 ,  Y02A40/146

Abstract: 본 발명은 식물의 바이오틴 생합성 과정에 관여하는 신규 폴리펩티드 및 이를 암호화하는 폴리뉴클레오티드, 그리고 상기 폴리펩티드의 발현 또는 기능을 억제하여 바이오틴 생합성을 저해함으로써 식물의 생장 억제를 유발하는 방법에 관한 것이다. 바이오틴 생합성 과정은 식물의 생장에는 필수적이나, 동물 및 인간에게는 존재하지 않는다. 따라서, 식물의 바이오틴 생합성 과정에 관여하는 본 발명의 신규 폴리펩티드의 발현 또는 기능을 억제하는 물질은 동물 및 인간에게는 무해한 새로운 제초제로 이용될 수 있다.

公开(公告)号：KR100508496B1

公开(公告)日：2005-08-17

申请号：KR1020030004230

申请日：2003-01-22

Applicant: 한국화학연구원

Inventor： 김범태 ,  이연수 ,  민용기 ,  박노균 ,  김진철

IPC: C07C69/76

Abstract: 본 발명은 살균 활성이 우수하고 독성이 낮으며 약효의 지속성이 개선된, 하기 화학식 1의 신규의 프로페노익 에스테르 및 아미드 유도체, 이의 제조방법 및 이를 포함하는 살균제 조성물에 관한 것이다.

상기 식에서,
Z는 F 또는 WR이고,
W는 O 또는 S이고,
R은 C
1 -C
4 알킬, 할로겐으로 치환된 C
1 -C
4 알킬, 또는 할로겐, 아실, 아미노, 니트로, 시아노, 아미노, 히드록시 또는 아실옥시로 치환된 아릴 또는 헤테로아릴이고;
Z가 F인 경우 X는 CH 또는 N이고, Y는 O 이며;
Z가 WR인 경우 X는 CH 또는 N이고, Y는 O 또는 NH이다.

公开(公告)号：KR1020050080452A

公开(公告)日：2005-08-12

申请号：KR1020050056454

申请日：2005-06-28

Applicant: 주식회사 오스코텍 ,  한국화학연구원

Inventor： 김정근 ,  김세원 ,  오귀옥 ,  고선일 ,  김종여 ,  이병의 ,  김범태 ,  이연수 ,  민용기 ,  박노균

IPC: A23L1/29 ,  A61K31/34

CPC classification number: A61K31/34 ,  A23L33/10 ,  A23L33/15 ,  A23L33/16 ,  A61K31/341 ,  C07D307/68

Abstract: 본 발명은 퓨란 유도체 및 그의 약학적으로 허용가능한 염을 함유하는 골다공증 예방 및 치료용 식품 조성물에 관한 것으로, 더욱 구체적으로 하기 화학식 1로 표시되는 퓨란 유도체는 종래 골다공증 치료제에 비해 골 증식 효과가 우수할 뿐만 아니라 부작용이 적어 골질환 예방 및 치료를 위한 의약품 또는 기능성 식품으로 사용할 수 있다.
화학식 1

(상기 식에서, X 및 Y는 하기 명세서에서 정의한 바와 같다.)

公开(公告)号：KR100467979B1

公开(公告)日：2005-01-27

申请号：KR1020040021097

申请日：2004-03-29

Applicant: 한국화학연구원

Inventor： 김범태 ,  민용기 ,  이연수 ,  박노균

IPC: C07D239/36

Abstract: PURPOSE: A fluorine-substituted heterocyclic compound as an intermediate for synthesis of agrochemicals and medicaments and a method for preparing the same are provided, thereby regio-selectively preparing the 5-fluoro-pyrazol derivative and 4-fluoro-6-hydroxy pyrimidine derivative in higher yield. CONSTITUTION: A method for preparing a 4-fluoro-6-hydroxy pyrimidine derivative with substituted phenyl at C3 or C4 position represented by the formula(2) comprises reacting a methyl 2-fluoroalkyl 2-phenylacetate derivative of the formula(3) with a substituted guanidine derivative(R2C(NH2)=NH) in the presence of an solvent, wherein X is hydrogen, halogen, C1-4 alkyl, C1-4 alkoxy or C1-4 arylalkyloxy; RF is fluorine or trifluoromethyl; R3 is hydrogen, C1-4 alkyl, C1-4 aryl or C1-4 arylalkyl; the solvent is acetonitrile, 1,4-dioxane, or 5 to 30 % 1,4-dioxane solution; and the reaction temperature is 60 to 120 deg. C.

Abstract translation: 目的：提供一种氟取代的杂环化合物作为合成农用化学品和药物的中间体及其制备方法，由此区域选择性地制备5-氟 - 吡唑衍生物和4-氟-6-羟基嘧啶衍生物 收益率较高。 构成：制备式（2）代表的在C3或C4位置上具有取代的苯基的4-氟-6-羟基嘧啶衍生物的方法包括使式（3）的2-氟代烷基2-苯基乙酸甲酯衍生物与 （R 2 C（NH 2）= NH），其中X是氢，卤素，C 1-4烷基，C 1-4烷氧基或C 1-4芳基烷氧基; RF是氟或三氟甲基; R3是氢，C1-4烷基，C1-4芳基或C1-4芳烷基; 溶剂为乙腈，1,4-二氧六环或5-30％1,4-二氧六环溶液; 反应温度为60〜120℃。 C。

公开(公告)号：KR100459938B1

公开(公告)日：2004-12-03

申请号：KR1020010063681

申请日：2001-10-16

Applicant: 한국화학연구원

Inventor： 김범태 ,  민용기 ,  이연수 ,  박노균

IPC: C07D231/20

Abstract: PURPOSE: Provided are a fluorine-substituted heterocyclic compounds, 5-fluorpyrazole derivative and 4-fluor-6-hydroxy pyrimidine, useful as intermediates for the synthesis of agrochemicals and medicinal antagonists and methods for preparing them regio selectively in high yields. CONSTITUTION: The fluorine-substituted heterocyclic compounds, 5-fluorpyrazole derivative and 4-fluor-6-hydroxy pyrimidine are represented by the formula(1a) or(1b), and formula(2) respectively, wherein X is hydrogen, halogen, C1-4 alkyl, C1-4 alkoxy or C1-C4 arylalkyloxy; RF is fluorine or trifluoromethyl; and R1, R2 and R3 are individually hydrogen, C1-4 alkyl, C1-4 aryl or C1-4 arylalkyl. They are manufactured by one pot reaction with a substituted hydrazine derivative and a guanidine derivative using methyl 2-fluoralkyl 2-phenylacetate derivative as a starting material.

Abstract translation: 用途：提供了用作合成农用化学品和药物拮抗剂的中间体的氟取代的杂环化合物，5-氟吡唑衍生物和4-氟-6-羟基嘧啶，以及以高产率选择性地制备它们的方法。 构成：氟取代的杂环化合物5-氟吡唑衍生物和4-氟-6-羟基嘧啶分别由式（1a）或（1b）和式（2）表示，其中X是氢，卤素，C1 -4烷基，C 1-4烷氧基或C 1 -C 4芳基烷氧基; RF是氟或三氟甲基; 且R1，R2和R3分别为氢，C1-4烷基，C1-4芳基或C1-4芳烷基。 它们通过使用甲基2-氟代烷基2-苯基乙酸酯衍生物作为原料通过与取代的肼衍生物和胍衍生物一锅法反应来制备。

公开(公告)号：KR1020040067218A

公开(公告)日：2004-07-30

申请号：KR1020030004230

申请日：2003-01-22

Applicant: 한국화학연구원

Inventor： 김범태 ,  이연수 ,  민용기 ,  박노균 ,  김진철

IPC: C07C69/76

Abstract: PURPOSE: Propenoic ester and amide derivatives having a fluorostyrene substituent, a process for preparing the same compounds and an antifungal composition comprising the same compounds are provided, which compounds have improved antifungal activity at a low concentration, wide range of antifungal activity, low toxicity and improved duration of medicine efficacy. CONSTITUTION: The propenoic ester and amide derivatives represented by formula (1) are provided, wherein Z is F or WR; W is O or S; R is C1-C4 alkyl, halogen substituted C1-C4 alkyl, or aryl or heteroaryl substituted with halogen, acyl, amino, nitro, cyano, hydroxy or acyloxy; and X is CH or N and Y is O when Z is F or X is CH or N and Y is O or NH when Z is WR. The process for preparing the propenoic ester and amide derivatives of formula (1) comprises the steps of: reacting bromide of formula (2) with 3-hydroxybenzaldehyde in the presence of base to prepare a compound of formula (3); and Wittig reacting the compound of formula (3) to prepare propenoic ester of formula (1a).

Abstract translation: 目的：提供具有氟苯乙烯取代基的丙烯酯和酰胺衍生物，制备相同化合物的方法和包含相同化合物的抗真菌组合物，该化合物在低浓度，广泛的抗真菌活性范围，低毒性下具有改善的抗真菌活性， 提高药效持续时间。 构成：提供由式（1）表示的丙烯酸酯和酰胺衍生物，其中Z是F或WR; W为O或S; R是C 1 -C 4烷基，卤素取代的C 1 -C 4烷基或被卤素，酰基，氨基，硝基，氰基，羟基或酰氧基取代的芳基或杂芳基; 当Z为F或X为CH或N且Y为O时，X为CH或N，Y为O，Z为WR时为Y。 制备式（1）的丙烯酸酯和酰胺衍生物的方法包括以下步骤：在碱的存在下使式（2）的溴与3-羟基苯甲醛反应以制备式（3）的化合物; （3）的化合物与维t嗪反应制备式（1a）的丙烯酸酯。

公开(公告)号：KR1020040043142A

公开(公告)日：2004-05-22

申请号：KR1020040021097

申请日：2004-03-29

Applicant: 한국화학연구원

Inventor： 김범태 ,  민용기 ,  이연수 ,  박노균

IPC: C07D239/36

Abstract: PURPOSE: A fluorine-substituted heterocyclic compound as an intermediate for synthesis of agrochemicals and medicaments and a method for preparing the same are provided, thereby regio-selectively preparing the 5-fluoro-pyrazol derivative and 4-fluoro-6-hydroxy pyrimidine derivative in higher yield. CONSTITUTION: A method for preparing a 4-fluoro-6-hydroxy pyrimidine derivative with substituted phenyl at C3 or C4 position represented by the formula(2) comprises reacting a methyl 2-fluoroalkyl 2-phenylacetate derivative of the formula(3) with a substituted guanidine derivative(R2C(NH2)=NH) in the presence of an solvent, wherein X is hydrogen, halogen, C1-4 alkyl, C1-4 alkoxy or C1-4 arylalkyloxy; RF is fluorine or trifluoromethyl; R3 is hydrogen, C1-4 alkyl, C1-4 aryl or C1-4 arylalkyl; the solvent is acetonitrile, 1,4-dioxane, or 5 to 30 % 1,4-dioxane solution; and the reaction temperature is 60 to 120 deg. C.

Abstract translation: 目的：提供作为农药和药物合成中间体的氟取代杂环化合物及其制备方法，从而选择性地制备5-氟 - 吡唑衍生物和4-氟-6-羟基嘧啶衍生物 更高的产量。 构成：由式（2）表示的在C3或C4位上制备具有取代苯基的4-氟-6-羟基嘧啶衍生物的方法包括使式（3）的2-氟代烷基2-苯基乙酸酯衍生物与 取代的胍衍生物（R2C（NH2）= NH）在溶剂存在下，其中X是氢，卤素，C 1-4烷基，C 1-4烷氧基或C 1-4芳烷氧基; RF是氟或三氟甲基; R3是氢，C1-4烷基，C1-4芳基或C1-4芳基烷基; 溶剂为乙腈，1,4-二恶烷或5-30％1,4-二恶烷溶液; 反应温度为60〜120℃。 C。

公开(公告)号：KR1020040035559A

公开(公告)日：2004-04-29

申请号：KR1020030072536

申请日：2003-10-17

Applicant: 주식회사 오스코텍 ,  한국화학연구원

Inventor： 김정근 ,  김세원 ,  오귀옥 ,  고선일 ,  김종여 ,  이병의 ,  김범태 ,  이연수 ,  민용기 ,  박노균

IPC: C07D307/56

CPC classification number: A61K31/34 ,  A23L33/10 ,  A23L33/15 ,  A23L33/16 ,  A61K31/341 ,  C07D307/68

Abstract: PURPOSE: Furan derivatives and pharmaceutical compositions for preventing and treating osteoporosis containing the same are provided, which improve the growth and activity of osteoblast, and inhibit the growth and activity of osteoclast, so that they can be useful for preventing and treating osteoporosis, as well as which have no toxicity, so that they can be used in foods. CONSTITUTION: Furan derivatives represented by the formula(1) or pharmaceutically acceptable salts thereof are provided, wherein X is H, OH, OR or NR1 R2; Y is OR, NR1R2, SC(=NH2)NH; R is hydrogen, naphthalene, or C1 to C4 aliphatic alkyl substituted with aryl having 3 or less substituents or proline having 4 or less substituents selected from methyl, methoxy, chloro, bromo, iodo, nitro and proline; and R1 and R2 are independently hydrogen, naphthalene, or aryl having 3 or less substituents selected from methyl, methoxy, chloro, bromo, iodo, nitro and proline, or C1 to C3 aliphatic alkyl, or R1 and R2 are aliphatic alkyl having the structure having carbon, oxygen or hydrogen or C1 to C3 aliphatic alkyl and nitrogens are connected together.

Abstract translation: 目的：提供用于预防和治疗含有此类骨质疏松症的呋喃衍生物和药物组合物，其改善成骨细胞的生长和活性，并抑制破骨细胞的生长和活性，从而可用于预防和治疗骨质疏松症 因为它们没有毒性，因此它们可以用于食物。 构成：提供由式（1）表示的呋喃衍生物或其药学上可接受的盐，其中X为H，OH，OR或NR 1 R 2; Y是OR，NR1R2，SC（= NH2）NH; R为氢，萘或被具有3个或更少取代基的芳基取代的C 1至C 4脂族烷基或具有4个或更少选自甲基，甲氧基，氯，溴，碘，硝基和脯氨酸的取代基的脯氨酸; R 1和R 2独立地是氢，萘或具有3个或更少的选自甲基，甲氧基，氯，溴，碘，硝基和脯氨酸的取代基的芳基或C1-C3脂族烷基，或R1和R2是具有结构 具有碳，氧或氢或C1至C3脂族烷基和氮连接在一起。

公开(公告)号：KR1020040003341A

公开(公告)日：2004-01-13

申请号：KR1020020038011

申请日：2002-07-02

Applicant: 제노마인(주) ,  한국화학연구원

Inventor： 이동희 ,  고재흥 ,  김태훈 ,  박유신 ,  조광연 ,  황인택 ,  최정섭 ,  민용기 ,  김태준 ,  이선우

IPC: C12N9/10

CPC classification number: C12N9/1029 ,  C12N15/8261 ,  C12N15/8263 ,  C12N15/8274 ,  Y02A40/146

Abstract: PURPOSE: A plant polypeptide having KAPA synthase function and a method for inducing plant growth inhibition and plant death by inhibiting the expression of the same are provided, thereby inhibiting the biotin biosynthesis, so that it can inhibit the plant growth and cannot affect human and animals. CONSTITUTION: A plant polypeptide having KAPA synthase function has the amino acid sequence of SEQ ID NO: 2, wherein the polypeptide is isolated from Arabidopsis thaliana; and the polypeptide contains aminotransferase class I and II domain at the C-terminal. A polynucleotide encoding the plant polypeptide has the nucleotide sequence of SEQ ID NO: 1. A recombinant vector containing the polynucleotide of SEQ ID NO: 1 is provided, wherein the vector is pCKAPA. A transformed E. coli(KCTC 10210BP) produced with the recombinant vector is provided. An antisense polynucleotide to the polynucleotide of SEQ ID NO: 1 is provided. A recombinant vector containing the antisense polynucleotide is provided, wherein the vector is pSEN-K. A transformant(KCTC 10211BP) produced with the recombinant vector is provided. A method for plant growth inhibition and plant death comprises inhibiting the expression of polypeptide and inhibiting the biotin biosynthesis, wherein the inhibition of the polypeptide expression is accomplished by antisense polynucleotide insertion, gene deletion, gene insertion, T-DNA insertion, homologous recombination or transposon tagging.

Abstract translation: 目的：提供具有KAPA合成酶功能的植物多肽和通过抑制其表达诱导植物生长抑制和植物死亡的方法，从而抑制生物素生物合成，从而可抑制植物生长并且不影响人和动物 。 构成：具有KAPA合成酶功能的植物多肽具有SEQ ID NO：2的氨基酸序列，其中所述多肽从拟南芥中分离; 并且该多肽在C-末端含有氨基转移酶I类和II型结构域。 编码植物多肽的多核苷酸具有SEQ ID NO：1的核苷酸序列。提供了含有SEQ ID NO：1的多核苷酸的重组载体，其中载体是pCKAPA。 提供用重组载体产生的转化的大肠杆菌（KCTC 10210BP）。 提供了与SEQ ID NO：1的多核苷酸的反义多核苷酸。 提供了含有反义多核苷酸的重组载体，其中载体是pSEN-K。 提供用重组载体产生的转化体（KCTC 10211BP）。 用于植物生长抑制和植物死亡的方法包括抑制多肽的表达和抑制生物素生物合成，其中多肽表达的抑制通过反义多核苷酸插入，基因缺失，基因插入，T-DNA插入，​​同源重组或转座子 标记。

公开(公告)号：KR1020030031795A

公开(公告)日：2003-04-23

申请号：KR1020010063681

申请日：2001-10-16

Applicant: 한국화학연구원

Inventor： 김범태 ,  민용기 ,  이연수 ,  박노균

IPC: C07D231/20

Abstract: PURPOSE: Provided are a fluorine-substituted heterocyclic compounds, 5-fluorpyrazole derivative and 4-fluor-6-hydroxy pyrimidine, useful as intermediates for the synthesis of agrochemicals and medicinal antagonists and methods for preparing them regio selectively in high yields. CONSTITUTION: The fluorine-substituted heterocyclic compounds, 5-fluorpyrazole derivative and 4-fluor-6-hydroxy pyrimidine are represented by the formula(1a) or(1b), and formula(2) respectively, wherein X is hydrogen, halogen, C1-4 alkyl, C1-4 alkoxy or C1-C4 arylalkyloxy; RF is fluorine or trifluoromethyl; and R1, R2 and R3 are individually hydrogen, C1-4 alkyl, C1-4 aryl or C1-4 arylalkyl. They are manufactured by one pot reaction with a substituted hydrazine derivative and a guanidine derivative using methyl 2-fluoralkyl 2-phenylacetate derivative as a starting material.

Abstract translation: 目的：提供氟代取代的杂环化合物，5-氟吡唑衍生物和4-氟-6-羟基嘧啶，其可用作合成农药和药物拮抗剂的中间体以及以高产率选择性地制备它们的方法。 构成：氟取代的杂环化合物，5-氟吡唑衍生物和4-氟-6-羟基嘧啶分别由式（1a）或（1b）和式（2）表示，其中X是氢，卤素，C1 -4-烷基，C 1-4烷氧基或C 1 -C 4芳基烷氧基; RF是氟或三氟甲基; 并且R 1，R 2和R 3分别是氢，C 1-4烷基，C 1-4芳基或C 1-4芳烷基。 它们通过与取代的肼衍生物和胍衍生物的一锅反应制备，使用2-苯基乙酸2-氟烷基酯衍生物作为起始原料。