Abstract:
본 발명은 하기 화학식 1로 표시되는 신규 페닐아세테이트 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 함유하는 T-형 칼슘 이온 채널의 활성에 의해 유발되는 질환의 예방 또는 치료용 조성물에 관한 것으로, 본 발명에 따른 페닐아세테이트 유도체를 함유하는 조성물은 T-형 칼슘 이온 채널 활성을 효과적으로 억제하므로 T-형 칼슘 이온 채널의 활성에 의해 유발되는 고혈압, 암, 간질, 신경성 통증 등의 질병의 예방 또는 치료제로서 유용하게 사용될 수 있다. [화학식 1] . (상기 화학식 1에서, 상기 X, R 1 및 R 2 는 본 명세서에서 정의된 바와 같다.) T-형 칼슘 채널 블로커, 페닐아세테이트 유도체, 통증치료제
Abstract:
PURPOSE: A method for preparing 1,6-dioxecane compound is provided to enlarge other ring by Diels-Alder reaction and to use as an intermediate. CONSTITUTION: A 1,6-Dioxecanes compound is denoted by chemical formula 1. The 1,6-Dioxecanes compound is prepared by Prins reaction of alcohol compound of chemical formula 2 and aldehyde compound of chemical formula 3. A tetrahydrofuran is used as a reaction catalyst. The reaction temperature is -78 to 30°C.
Abstract:
PURPOSE: A thiazoline compounds and a T-type calcium channel inhibitor containing the same are provided to treat diseases relating to T-type calcium channel overexpression. CONSTITUTION: A thiazoline compounds have a structure of chemical formula 1. A composition for preventing and treating diseases relating to T-type calcium channel overexpression contains the thiazoline compounds of chemical formula 1. The diseases are Parkinson's disease, Alzheimer, schizophrenia, somnopathy, pain, hypertension, arrhythmia, angina, cardiac insufficiency, myocardial infarction, or cancer.
Abstract:
PURPOSE: A novel phenylacetate derivative and a composition containing the same are provided to suppress T-type calcium ion channel activity and to use as a therapeutic agent for preventing or treating diseases caused by T-type calcium ion channel activity. CONSTITUTION: A phenylacetate derivative is denoted by chemical formula 1. A method for preparing the phenylacetate derivative comprises: a step of performing esterification of a carboxylic acid compound of chemical formula 2 under acid catalyst to obtain an ester compound of chemical formula 3; a step of reacting the compound of chemical formula 3 with t-butoxide and isopropyl bromide to obtain a compound of chemical formula 4; a step of reacting the compound of chemical formula 4 with 1,3-dibromopropane to obtain a compound of chemical formula 5; and a step of reacting the compound of chemical formula 5 with a compound of chemical formula 6 or 7.
Abstract:
본 발명은 1-(2-하이드록시페닐)부타-2-엔-1-온 또는 크로만-4-온 유도체의 제조방법에 관한 것으로서, 더욱 상세하게는 2-에티이닐페놀 유도체를 루이스산 촉매 존재 하에서 알데하이드 화합물과 반응시켜 하기 화학식 1로 표시되는 1-(2-하이드록시페닐)부타-2-엔-1-온 유도체 또는 하기 화학식 2로 표시되는 크로만-4-온 유도체를 제조하는 방법에 관한 것이다.
상기 화학식 1 또는 2에서, R 1 및 R 2 는 각각 발명의 상세한 설명에서 정의한 바와 같다. 1-(2-하이드록시페닐)부타-2-엔-1-온, 크로만-4-온, 루이스산
Abstract:
PURPOSE: Provided are chiral diphosphine compounds which form a metal complex with transition metal thus have excellent optical selectivity and transition rate, and a manufacturing method of chiral compounds by applying them as metal catalyst in asymmetric reactions. CONSTITUTION: The chiral diphosphine compound is represented by the formula(1), wherein X, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R10 and R11 are as defined in the description. It is characteristically manufactured by a compound of the formula(7) with an organophosphine-based metallic salt of the formula(8) in the presence of organic solvents.
Abstract:
PURPOSE: Provided are a water soluble chiral auxiliary (5R,5'R)-5,5'-bis(oxazolidin-2-one) and its synthetic process, thereby synthesizing 2 equivalent of chiral compounds using 1 equivalent of chiral auxiliary agent and removing high cost of chiral auxiliary agent from organic reaction products. CONSTITUTION: The water soluble chiral auxiliary (5R,5'R)-5,5'-bis(oxazolidin-2-one) is represented by the formula(1). It is manufactured by the steps of: hydrogenation debenzylating 1,4-dibenzyl-2,3-dimethylsulfonyl tetrahydroxy butane under hydrogen atmosphere of 1 atm, to prepare (2S,3S)-2,3-bis(O-methanesulfonyl)-1,2,3,4-tetrahydroxy butane; heating and refluxing (2S,3S)-2,3-bis(O-methanesulfonyl)-1,2,3,4-tetrahydroxy butane and benzyl isocyanate to prepare (5R,5R')-N,N'-dibenzyl-5,5'-bis(oxazolidin-2-on) under sodium hydride; and debenzylating (5R,5R')-N,N'-dibenzyl-5,5'-bis(oxazolidin-2-on) using liquid ammonia and sodium metal to obtain (5R,5'R)-5,5'-bis(oxazolidin-2-one) of the formula(1).
Abstract:
PURPOSE: A process for preparing an optical active aminoalcohol compound using a cinchona alkaloid catalyst having excellent catalytic performance, reusable and excellent in thermal, mechanical stability, a nitrogen source and a base is provided which carries out the heterogeneous asymmetric aminohydroxylation of olefins economically and can improve processing difficulties by high toxicity and volatility of OsO4. CONSTITUTION: In the process for manufacturing an optical active aminoalcohol compound by heterogeneous asymmetric aminohydroxylation of olefins, the process uses a catalytic system containing conventional cinchona alkaloids of formula 1 and a nitrogen source and a base. In formula, Y is hydroquinidinyl represented by formula 2 or hydroquinidinyl represented by formula 3, X represents an unsaturated compound containing 0 or 4 carbons, pyridazine in case X is 0 and phthalazine in case X is an unsaturated compound, R represents methoxy, ethoxy or methyl.
Abstract:
본 발명은 출발물질로서 다음 구조식(Ⅱ)의 (R)-4(트리클로로메틸)옥세탄-2-온을 산 촉매하에 C 1 -C 18 지방족 알코올 또는 벤질알코올과 반응시켜 다음 일반식(Ⅲ)의 (R)-3-히드록시-4,4,4-트리클로로부티르산 에스테르를 제조한 다음, 일반식(Ⅲ)의 화합물의 4-위치를 선택적으로 탈염소화(Bis-dechlorination)시키는 것으로 이루어진 다음 일반식(Ⅰ)의 (R)-3-히드록시-4-클로로부티르산 에스테르의 제조방법에 관한 것이다.
상기식에서 R은 C 1 -C 18 의 지방족 알킬기 또는 벤질기이다. 본 발명의 제조방법은 (R)-카르니틴 또는 (R)-3-히드록시-4-아미노부티르산의 제조에 이용되는 핵심 중간체인 (R)-3-히드록시-4-클로로부티르산 에스테르를 매우 높은 수율로 또한 광학적으로 순수한 형태로 얻을 수 있다.