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β-Difluoro-α-trimethylsilyl-γ-lactam 유도체의 합성
채규윤,곽경철,문재정,최장호 圓光大學校 基礎自然科學硏究所 2000 基礎科學硏究誌 Vol.18 No.1
α-위치만 선택적으로 difluoromethylene기가 도입된 α.α-difluoro-γ-trimethylsilyl-γ-lactam 유도체(6)들은 ethyl α.α-difluoro-γ-trimethylsilyl-γ-iodopentanoate(4)는 일차아민 유도체와의 반응으로부터 비교적 편리한 작용조건과 비교적 좋은 수득률로 합성하였다. The target of α.α-difluoro-γ-trimethylsilyl-γ-lactam derivatives(6) with selectively in corporated difluoromethylene on α-position were readily prepared form reaction ethyl α.α-difluoro-γ-trimethylsilyl-γ-iodopentanoate(4) and primary derivatives in moderate yields.
鄭起源,蔡奎允,李英行 圓光大學校 1993 論文集 Vol.27 No.2
새로운 축합시약인 (3-nitropyridyl) dialkyl phosphate (3a,3b)를 2-hydroxy-3-nitropyridine (1), dialkyl chlorophosphate (2a,2b) 그리고 triethylamine을 dichloromethane 용액중에서 1시간동안 상온에서 반응시켜 쉽게 얻을 수 있었다. 축합시약인 3a와 3b는 온화한 반응 조건에서 아미드와 디펩티드를 합성하는데 있어서 유용한 시약임을 알 수 있었다. A new coupling reagents,(3-nitropyridyl) diallkyl phosphate (3a,3b), were readily prepared by the reaction of 2-hydroxy-3-nitropyridine (1), dialkyl chlorophosphate (2a,2b), and triethylamine in dichloromethane at room temperature for 1h. The coupling reagents, 3a and 3b, were found to be very useful for the preparation of amides and dipeptides under mild conditions.
Synthesis of 6-Alkyloxyl-3,4-dihydro-2(1H)-quinoliones and Their Anticonvulsant Activities
Kyu-Yun Chai,Jun-Min Wang,노정래,Kyung-Chell Kwak,Hee-Cheol Kang,Chang-Soo Jun,Zhe-Shan Quan 대한화학회 2005 Bulletin of the Korean Chemical Society Vol.26 No.11
A series of 6-alkyloxyl-3,4-dihydro-2(1H)-quinoliones (5a-5n) were synthesized through nitration, reduction, diazotization, hydrolysis and alkylation from 3,4-dihydro-2(1H)-quinolione. Their structures were characterized by IR, 1H-NMR and MS. The anticonvulsant activity was evaluated by the Maximal electroshock test (MES) and the subcutaneous pentylenetetrazole (Metrazole) test (sc-Met). The neurotoxicity was measured by the Rotarod test (Tox). The result showed that 6-hexyloxy-3,4-dihydro-2 (1H)-quinolinone (5c) was potent in anti-MES and anti-scMet test with ED50 of 24.0 mg/kg and 21.2 mg/kg, respectively, albeit its TD50 (67.6 mg/kg) revealed the high neurotoxicity. 6-Benzyloxy-3,4-dihydro-2(1H)-quinolinone (5f) was less effective against MES induced seizure with ED50 of 29.6 mg/kg, but no neurotoxicity was observed even under 300 mg/kg. Its Protective index (PI) was greater than 10 preferable to Phenytoin, Carbamazepin, Phenobarbital and Valproate.
Scutellaria baicalensis Inhibits Mast Cell-Mediated Anaphylactic Reactions
Yun Ho Choi(최윤호),Eui-Hyeog Han(한의혁),Ok Hee Chai(채옥희),Yun-Kyu Kim(김윤규),Hyoung Tae Kim(김형태),Chang Ho Song(송창호) 대한체질인류학회 2010 대한체질인류학회지 Vol.23 No.4
비만세포는 즉시형 과민반응과 알레르기성 질환의 발현에 중요한 역할을 한다. 황금은 동양의학에서 전통적으로 널리 사용된 약초로, 약리작용에는 항암, 항바이러스, 항박테리아, 항염증 효과 등이 있다. 그러나, 황금이 비만세포를 매개로 한 아나필락틱 반응에 미치는 영향을 다룬 연구가 거의 없는 실정이다. 본 연구에서 우리는 황금의 메탄올 추출물이 compound 48/80 혹은 anti-DNP IgE에 의한 쥐 모델 아나필락시에 미치는 영향을 관찰하였다. 이러한 결과를 보다 확실히 입증하고자, 비만세포의 히스타민 유리에 초점을 맞춰서 황금이 이들 세포에 대해 억제효과를 보이는지 확인하였다. 황금은 compound 48/80에 의한 전신성 아나필락시양 반응과 그에 따른 혈장 내 히스타민 유리 그리고 귀의 부종반응을 억제하였다. 황금은 또한 anti-DNP IgE에 의해 수동적으로 유도된 전신 및 피부 아나필락시 반응을 억제하였다. 시험관 내 실험에서, 황금은 compound 48/80에 의해 유도된 비만세포의 탈과립을 억제하였으며, compound 48/80 혹은 anti-DNP IgE로 활성화된 비만세포로부터의 히스타민 유리를 감소시켰다. 이외에도 compound 48/80에 의해 유도된 세포 내 칼슘 유입이 황금에 의해 농도의존적으로 억제되었다. 아울러 황금은 일시적으로 비만세포 내 cAMP의 양을 증가시켰다. 이상의 결과들은 황금이 효과적인 항 아나필락틱 활성을 가지고 있음을 제시한다. Mast cells play a critical role in the effector phase of immediate hypersensitivity and allergic diseases. Scutellaria baicalensis is a widely used herb in traditional oriental medicine with anticancer, antiviral, antibacterial and anti-inflammatory properties. However, the roles of Scutellaria baicalensis in mast cell-mediated anaphylactic reactions have not fully been investigated. In this study, we examined the influences of the methanol extract of Scutellaria baicalensis (MESB) on compound 48/80- or anti-dinitrophenyl (DNP) IgE-induced anaphylaxis-like response in vivo. To further prove these in vivo results, the inhibitory effect of MESB on mast cell activation was evaluated, focusing on the histamine release from rat peritoneal mast cells (RPMC). MESB inhibited compound 48/80-induced systemic anaphylaxis-like reaction, plasma histamine release and ear swelling response in mice. MESB also attenuated passive systemic and cutaneous anaphylaxis evoked by anti-DNP IgE. In in vitro experiments, MESB dose-dependently reduced histamine release from RPMC activated by compound 48/80 or anti-DNP IgE. Moreover, compound 48/80-elicited calcium uptake was suppressed in a concentration-dependent manner of MESB. Furthermore, MESB transiently increased the level of intracellular cAMP. From these results, it is suggested that MESB possesses effective anti-anaphylactic activity.
Diethyl-2-carbamoyl-2,3-difluoroethenephosphonate의 합성에 관한 연구
채규윤 圓光大學校 基礎自然科學硏究所 1997 基礎科學硏究誌 Vol.16 No.1
Diethyl(2-carbarmoy1-2,3-difluoro ethenyl)phosphonates were prepared by the reaction Ethyl(1,1,2,3,3-pentafluoro-3-propenyl)phosphonate(3) with piperdine or benzylamine in the pnesence water.
Ethyl-4-fluoro-5-phenylpyrrole-2-carboxylate 유도체의 효율적인 합성법
채규윤 圓光大學校 基礎自然科學硏究所 1997 基礎科學硏究誌 Vol.16 No.1
Ethyl-4-fluoro-1-methyl-5-phenylpyrrole-2-carboxylate was synthesized in high yield by the reaction of α,α-difluoro-γ-iodomethylketone and methyl amine. providing: a new: simple, and efficient method for the syntheis of Ethyl-4-fluoro-1-methyl-5-phenylpyrrole-2-carboxylate
3-Perfluoroalkyl-1-propene의 합성
채규윤 圓光大學校 基礎自然科學硏究所 1997 基礎科學硏究誌 Vol.16 No.1
3-Perfluoroalkyl-1-propene were prepared easily by the reaction perfluoroalkyl iodide with allytrimethylsilane in presmie catalystic amount(5 mole %) pd[p(ph_3)]_4.
채규윤 圓光大學校 基礎自然科學硏究所 1997 基礎科學硏究誌 Vol.16 No.1
β-Fluoropyrrole derivatives were synthesized by the reaction ethyl-5-phenyl-2-iodo-5-oxobutanoate with excess ammonium hydroxide.
N, 3-Diphenyl-4,4-difluoro-5-benzyl-4,5-difluoropyrazole의 합성에 관한 연구
채규윤 圓光大學校 基礎自然科學硏究所 1997 基礎科學硏究誌 Vol.16 No.1
N-3-Diphenyl-4,4-difluoro-5benzyl-4,5-difluoropyrazole(4) was sythesized from the reaction of 3-hydraxy-1,4-diphenyl-1-butanone and phenylhydrazine.