公开(公告)号：KR100141068B1

公开(公告)日：1998-07-01

申请号：KR1019940022095

申请日：1994-09-02

Applicant: 한국과학기술연구원

Inventor： 김유승 ,  강순방

IPC: C12P7/22

Abstract: 본 발명은 3(R)-메틸-[1,4]-벤즈옥사진 유도체를 출발 물질로하여 100 내지 160℃에서 1 내지 4시간 동안 폴리인산과 반응시키는 것을 특징으로 하는 (+)3(R)-메틸피리도벤즈옥사진 카르복실레이트 유도체의 제조 방법에 관한 것으로서, 이 제조 방법에서 출발 물질로 사용되는 3(R)-메틸-[1,4]-벤즈옥사진 유도체는 2-(2(S)-케토프로필옥시)니트로벤젠 유도체를 베이커 이스트와 당류 존재하에 물과 알콜 용매 중에서 25 내지 50℃에서 4 내지 10시간 동안 가열 교반시켜 2-(2(S)-히드록시프로필옥시)니트로벤젠 유도체를 얻고, 이 화합물을 금속 촉매 존재하에 알콜 용매 중에서 2 내지 6시간 동안 1기압의 수소와 반응시켜 2-(2(S)-피드록시프로필옥시)아닐린 유도체를 얻고, 이 화합물을 에탄올 용매 중에서 100 내지 160℃에서 5 내지 10시간 동안 알킬 에록시메틸렌말로네이 트와 반응시켜 N-(2,2-디에록시카르보닐에테닐)-2-(2(S)-히드록시프로필옥시)아닐린 유도체를 얻고, 이 화합물을 유기 용매 중에서 -10 내지 10℃에서 1 내지 4 시간 동안 트리페닐포스핀 및 디에틸아조디카르복실레이트와 반응시킴으로써 제조할 수 있다.

公开(公告)号：KR100125115B1

公开(公告)日：1997-12-05

申请号：KR1019940005762

申请日：1994-03-22

Applicant: 한국과학기술연구원

Inventor： 김유승 ,  강순방 ,  박선희

IPC: C07D498/04

CPC classification number: C07D498/06

Abstract: The piperazine benzoxazine derivatives(I; R, R1, R2= H, C1-4 alkyl), useful as an antibacterial agent, were prepared by the reaction of (-)benzoxazine derivatives(III) and piperazine derivatives(IV; R1, R2= H, C1-4 alkyl; Z= H, trialkylsilyl) at 60- 80 deg.C for 2- 3 hours in an organic solvent in the presence of a mixture of tetraalkylammonium halide, tetraammonium halide and metal fluoride. The derivatives(III) were prepared by the reaction of (+)-aminomethylene-3-oxo-3- phenylpropionate derivatives(II; X= halogen atom; X1, X2= halogen atom, nitro group; R3, R4= C1-4 alkyl) and a base such as metal hydroxide or metal hydride at 50- 150 deg.C for 2- 24 hours in an organic polar solvent such as acetonitrile, dimethylacetamide, etc. and water.

Abstract translation: 通过（ - ）苯并恶嗪衍生物（III）和哌嗪衍生物（IV; R1，R2）的反应制备可用作抗菌剂的哌嗪苯并恶嗪衍生物（I; R，R1，R2 = H，C1-4烷基） = H，C 1-4烷基; Z = H，三烷基甲硅烷基），在有机溶剂中，在四烷基卤化铵，四卤化铵和金属氟化物的混合物存在下，在60-80℃下反应2-3小时。 衍生物（III）通过（+） - 氨基亚甲基-3-氧代-3-苯基丙酸酯衍生物（II; X =卤素原子; X1，X2 =卤素原子，硝基; R3，R4 = C1-4 烷基）和碱如金属氢氧化物或金属氢化物在50-150℃下在有机极性溶剂如乙腈，二甲基乙酰胺等和水中进行2-24小时。

公开(公告)号：KR1019950032236A

公开(公告)日：1995-12-20

申请号：KR1019940011748

申请日：1994-05-28

Applicant: 한국과학기술연구원

Inventor： 김유승 ,  강순방 ,  박선희

IPC: C07F7/10

Abstract: 본 발명은 박테리아에 살균 효과를 나타내는 강력한 항균제인 피리도벤즈옥사진 제조에 사용되는 중간체인 일반식(I)의 (+)2-벤조일-3-(실릴옥시프로피-2(S)-일) 아미노 아크릴레이트 유도체 제조방법에 관한 것이다.

일반식(I)에서 X는 불소 또는 염소원자, X
1 , X
2 는 할로겐원자 또는 니트로기, R
1 , R
2 , R
3 , R
4 는 탄소원자 1 내지 8개의 알킬 또는 아릴기를 나타낸다.
본 발명에서는 일반식(III)의 아크릴레이트 유도체와 일반식(IV)의 트리알킬실릴클로라이드를 염기 존재하에 유기용매 중에서 반응시켜 일반식(V)의 (+)실릴아크릴옥시아크릴레이트 유도체를 제조하고 일반식(V) (+)실릴옥시아크릴레이트 유도와 일반식(VI)의 벤조일클로라이드를 염기 존재하에 유기용매 중에서 반응시켜 일반식(I)의 화합물을 제조한다.

일반식(III),(IV),(V)에서 R
1 , R
2 , R
3 , R
4 는 탄소원자 1 내지 8개의 알킬 또는 아릴기를 나타내고, 일반식(IV)에서 X는 불소 또는 염소원자, X
1 , X
2 는 할로겐 또는 니트로기를 표시한다.

公开(公告)号：KR100053625B1

公开(公告)日：1992-08-06

申请号：KR1019900004115

申请日：1990-03-27

Applicant: 한국과학기술연구원

Inventor： 박상우 ,  김유승 ,  이진화

IPC: C07D401/04

公开(公告)号：KR1019910016736A

公开(公告)日：1991-11-05

申请号：KR1019900004115

申请日：1990-03-27

Applicant: 한국과학기술연구원

Inventor： 박상우 ,  김유승 ,  이진화

IPC: C07D401/04

Abstract: 내용 없음

公开(公告)号：KR1019900001079B1

公开(公告)日：1990-02-26

申请号：KR1019860008795

申请日：1986-10-20

Applicant: 한국과학기술연구원

Inventor： 박상우 ,  김유승

IPC: C07D215/22

Abstract: Quinolone derivs. of formula (I) are prepd. by reacting cpds. of formula (II) with EDTA in polar solvent(i.e. mixt. of water/MeOH and water/EtOH) in the presence of metal powder selected from a gp. of Zn, Cu, Mn or Fe and catalytic amt. of iodides(i.e. NaI, KI, CaI2) for 1-10 hr at 50-100 deg. C. In the formulas, R=H, Me, Et, propyl or butyl; X=Br; Z=Cl or piperazinyl gp.. (I) are useful as an antibacterial agent.

Abstract translation: 喹诺酮衍生物。 式（I）的化合物是制备的。 通过cpds反应。 式（II）与EDTA在极性溶剂（即水/ MeOH和水/ EtOH的混合物）中在金属粉末存在下，选自gp。 的Zn，Cu，Mn或Fe和催化剂。 的碘化物（即NaI，KI，CaI 2）在50-100℃下1-10小时。 式中，R = H，Me，Et，丙基或丁基; X = Br的; Z = Cl或哌嗪基gp（I）可用作抗菌剂。

公开(公告)号：KR1020100090979A

公开(公告)日：2010-08-18

申请号：KR1020090010234

申请日：2009-02-09

Applicant: 한국과학기술연구원

Inventor： 조용서 ,  김유승 ,  이재균 ,  민선준 ,  배애님 ,  추현아 ,  사티쉬샤브로

IPC: C07D307/90 ,  C07D307/93

Abstract: PURPOSE: An oxaspiro compound and a method for preparing the same are provided to be used as an intermediate in a natural product or novel drug synthesis. CONSTITUTION: An oxaspiro compound is denoted by chemical formula 1. In chemical formula 1, R1 and R2 are hydrogen, alkyl group of C1-C6, halogen, nitro, alkyl of C1-C6, or substituted or non-substituted phenyl group as a substituent of C1-C6 alkoxy. The oxaspiro compound of chemical formula 1 is prepared by reacting a carbo compound of chemical formula 3 with methylene cycloalkandiol of chemical formula 2 under the presence of lewis acid. The reaction solvent is dichloro methane. Trimethylsilyl trifluoromethansulfonate(TMSOTf) is used as the lewis acid.

Abstract translation: 目的：提供氧杂螺环化合物及其制备方法，用作天然产物或新药合成中的中间体。 化学式1中，R1和R2为氢，C1-C6烷基，卤素，硝基，C1-C6烷基或取代或未取代的苯基，为 C1-C6烷氧基的取代基。 化学式1的氧杂螺环化合物通过在路易斯酸存在下使化学式3的碳化合物与化学式2的亚甲基环二醇反应来制备。 反应溶剂是二氯甲烷。 三氯甲磺酸三甲基甲硅烷基酯（TMSOTf）用作路易斯酸。

公开(公告)号：KR1020090090224A

公开(公告)日：2009-08-25

申请号：KR1020080015550

申请日：2008-02-20

Applicant: 한국과학기술연구원

Inventor： 조용서 ,  김유승 ,  이재균 ,  추현아 ,  배애님 ,  사티쉬샤브로

IPC: C07D309/04

CPC classification number: C07D309/06

Abstract: A method for manufacturing a tetrahydropyran derivative is provided to produce an intermediate for synthesizing functional natural material using a homopropagylic alcohol derivative and aldehyde compound. A tetrahydropyran derivative having cis-substituent on C2 and C6 is denoted by the chemical formula 1. In the chemical formula 1, R1 and R2 are separately C1-C6 alkyl group, C6-C15 aryl C1-C6 alkyl group, or C6-C15 aryl group. A method for manufacturing the tetrahydropyran derivative comprises a step of performing prince reaction of aldehyde compound of the chemical formula 3 with homopropagylic alcohol derivative of the chemical formula 2 to produce dihydropyran-3-ilyden triplate compound of the chemical formula 1a.

Abstract translation: 提供四氢吡喃衍生物的制造方法，以制备使用高分子量醇衍生物和醛化合物合成官能天然材料的中间体。 化学式1表示在C2和C6上具有顺式取代基的四氢​​吡喃衍生物。在化学式1中，R 1和R 2分别是C 1 -C 6烷基，C 6 -C 15芳基C 1 -C 6烷基或C 6 -C 15 芳基。 四氢吡喃衍生物的制造方法包括使化学式3的醛化合物与化学式2的异丙醇衍生物进行王子反应的步骤，得到化学式1a的二氢吡喃-3-基锂化合物。

公开(公告)号：KR100758317B1

公开(公告)日：2007-09-13

申请号：KR1020060039225

申请日：2006-05-01

Applicant: 한국과학기술연구원

Inventor： 금교창 ,  김유승 ,  강순방 ,  임혜원 ,  장민석 ,  구일회

IPC: A61K31/5375 ,  A61P9/04

CPC classification number: A61K31/5375

Abstract: A composition for blocking T-type calcium channel comprising morpholin-2-one derivatives is provided to block the T-type calcium channel in the same level as the conventional T-type calcium channel blocker, mibefradil, without side effects. A composition for blocking T-type calcium channel comprises morpholin-2-one derivatives represented by the formula(1), or pharmaceutically acceptable salts thereof, wherein R^1 and R^2 are each independently hydrogen, C1-C6 alkyl, C1-C6 cycloalkyl, or phenyl optionally substituted by halogen, nitro, hydroxyl or C1-C6 alkoxy; and R^3 and R^4 are each independently hydrogen, C1-C6 alkyl, C1-C6 thioalkyl, amino or phenyl optionally substituted by halogen, nitro, hydroxyl or C1-C6 alkoxy. The composition prevents or treats diseases caused by overexpression of T-type calcium channel including angina pectoris, hypertension, myocardiac infarction, pain and epilepsy.

Abstract translation: 提供一种用于阻断包含吗啉-2-酮衍生物的T型钙通道的组合物，以阻断与常规T型钙通道阻滞剂米非司酮相同水平的T型钙通道，无副作用。 用于阻断T型钙通道的组合物包括由式（1）表示的吗啉-2-酮衍生物或其药学上可接受的盐，其中R 1和R 2各自独立地为氢，C 1 -C 6烷基， C 6环烷基或任选被卤素，硝基，羟基或C 1 -C 6烷氧基取代的苯基; R 3和R 4各自独立地为氢，C 1 -C 6烷基，C 1 -C 6硫代烷基，任选被卤素，硝基，羟基或C 1 -C 6烷氧基取代的氨基或苯基。 该组合物预防或治疗由过度表达T型钙通道引起的疾病，包括心绞痛，高血压，心肌梗塞，疼痛和癫痫。

公开(公告)号：KR1020030058740A

公开(公告)日：2003-07-07

申请号：KR1020010089274

申请日：2001-12-31

Applicant: 한국과학기술연구원

Inventor： 조용서 ,  김유승 ,  고훈영 ,  최경일 ,  강경호 ,  배애님

IPC: C07D215/56

Abstract: PURPOSE: Quinolone derivatives and a preparation process thereof are provided, thereby cheaply preparing quinolone derivatives under mild conditions. CONSTITUTION: Quinolone derivatives are represented by the formula 6, wherein R is H, or halogen selected from Cl, F, Br and I; R1 and R2 are independently H, alkyl or OH; and Y is -Ts(tosyl), -Ms(mesyl) or -Ac(acetyl). A process for preparing the quinolone derivatives of the formula 6 comprises the steps of: reacting a compound of the formula 1 with a compound of the formula 2 in the presence of indium metal and acid to simultaneously perform allylation of aldehyde and reduction of nitro group, thereby preparing a compound of the formula 3; protecting amine group of the compound of the formula 3 to prepare a compound of the formula 4; oxidizing secondary alcohol of the compound of the formula 4 to prepare a compound of the formula 5; and cyclization of the compound of the formula 5 in the presence of organic base, wherein the oxidation of secondary alcohol uses pyridinium chlorochromate(PCC) or pyridinium dichromate(PDC) or Swern's oxidation or Dess-Martin periodinane oxidation; and the organic base is diisopropylethylamine, DBU (1,8-diazabicyclo£5.4.0|undec-7-ene), DBN (1,5-diazabicyclo£4.3.0|non-5-ene), triethylamine or pyridine.

Abstract translation: 目的：提供喹诺酮衍生物及其制备方法，从而在温和条件下廉价制备喹诺酮衍生物。 组成：喹诺酮衍生物由式6表示，其中R是H，或选自Cl，F，Br和I的卤素; R1和R2独立地为H，烷基或OH; 和Y是-T（甲苯磺酰基），-Ms（甲磺酰）或-Ac（乙酰基）。 制备式6的喹诺酮衍生物的方法包括以下步骤：在铟金属和酸存在下使式1的化合物与式2的化合物反应，以同时进行醛的还原和烯丙基的还原， 从而制备式3的化合物; 保护式3化合物的胺基以制备式4的化合物; 氧化式4化合物的仲醇制备式5的化合物; 在有机碱的存在下环化式5的化合物，其中仲醇的氧化使用氯铬酸吡啶鎓（PCC）或重铬酸吡啶鎓（PDC）或Swern的氧化或Dess-Martin氧化氧化; 有机碱是二异丙基乙胺，DBU（1,8-二氮杂双环{5.4.0 |十一-7-烯），DBN（1,5-二氮杂双环{4.3.0 |非-5-烯），三乙胺或吡啶。