α, β-이노에이트 유도체의 제조방법
    61.
    发明公开
    α, β-이노에이트 유도체의 제조방법 有权
    α-YNOATE衍生物的制备方法

    公开(公告)号:KR1020120109929A

    公开(公告)日:2012-10-09

    申请号:KR1020110027843

    申请日:2011-03-28

    Abstract: PURPOSE: A manufacturing method of A, B-ynoate derivative is provided to manufacture A, B-ynoate derivatives with high yield through a cross coupling reaction of aryl halide derivative and organic indium under the presence of a palladium catalyst. CONSTITUTION: A manufacturing method of A, B-ynoate derivative comprises a step of preparing A, B-ynoate in chemical formula 1: R^2O2C≡R^1 by a cross coupling reaction of an aryl halide derivative in chemical formula 2: R^1-Ar-X and an organic indium specimen in chemical formula 3: [R^2O2C≡]4-InLi under the presence of a palladium catalyst and phosphine ligand. In the chemical formulas R^1 is hydrogen, (C1-C7)alkyl, (C1-C7) alkoxy, halogen, (C1-C7) alkoxycarbonyl, (C1-C7)alkylcarbonyl or *≡CO2R^3, R^2 and R^3 is respectively (C1-C7)alkyl, Ar is (C6-C20) arylene or (C3-C20)heteroarylene, and X is halogen.

    Abstract translation: 目的:提供A,B-ynoate衍生物的制备方法,通过芳基卤衍生物和有机铟的交叉偶联反应,在钯催化剂存在下,以高产率制备A,B-ynate衍生物。 构成:A,B-ynoate衍生物的制造方法包括通过化学式2中的芳基卤衍生物的交叉偶联反应制备化学式1中的A,B-ynate的步骤:R ^2O2C≡R^ 1:R 1-Ar-X和化学式3中的有机铟试样:[R 2 O 2C≡] 4-InLi,在钯催化剂和膦配体存在下。 在化学式中,R 1是氢,(C 1 -C 7)烷基,(C 1 -C 7)烷氧基,卤素,(C 1 -C 7)烷氧基羰基,(C 1 -C 7)烷基羰基或*≡CO2 R 3,R 2和 R 3分别为(C 1 -C 7)烷基,Ar为(C 6 -C 20)亚芳基或(C 3 -C 20)亚杂芳基,X为卤素。

    인듐을 이용한 알코올 유도체의 제조방법
    62.
    发明公开
    인듐을 이용한 알코올 유도체의 제조방법 有权
    使用印迹的醇合物衍生物的新合成

    公开(公告)号:KR1020120109928A

    公开(公告)日:2012-10-09

    申请号:KR1020110027842

    申请日:2011-03-28

    Abstract: PURPOSE: A manufacturing method of alcohol derivative is provided to reduce a use amount of metal, to obtain high yield at room temperature in short time, and to be suitable for manufacturing alcohol for medicine and perfume by using environmental-friendly isopropanol as a solvent and indium which has less toxicity as solvents. CONSTITUTION: A manufacturing method of alcohol derivative comprises: a step of preparing an alcohol derivative in chemical formula 1 by reacting an aldehyde derivative in chemical formula 2 and an indium alkoxide derivative in chemical formula 3. In chemical formula 1-3, R is (C1-C10)alkyl, (C3-C12) cycloalkyl, (C6-C12) aryl, (C3-C12)heteroaryl, a functional group in chemical formula (a) or a functional group in chemical formula (b), R^11-R^15 is independently hydrogen, halogen, (C1-C10)alkyl or (C3-C12)aryl, and R^1 and R^2 is (C1-C10)alkyl.

    Abstract translation: 目的:提供醇衍生物的制造方法以减少金属的使用量,在短时间内在室温下获得高产率,并且适合于通过使用环保的异丙醇作为溶剂来制造用于医药和香料的酒精, 铟作为溶剂具有较小的毒性。 构成:醇衍生物的制造方法包括:通过使化学式2中的醛衍生物与化学式3中的烷氧基铝衍生物反应,在化学式1中制备醇衍生物的步骤。在化学式1-3中,R为( C1-C10)烷基,(C3-C12)环烷基,(C6-C12)芳基,(C3-C12)杂芳基,化学式(a)中的官能团或化学式(b) -R 15独立地是氢,卤素,(C 1 -C 10)烷基或(C 3 -C 12)芳基,R 1和R 2是(C 1 -C 10)烷基。

    신규한 인돌리진 유도체와 이의 제조방법
    63.
    发明授权
    신규한 인돌리진 유도체와 이의 제조방법 有权
    新型中和衍生物及其制备方法

    公开(公告)号:KR101125531B1

    公开(公告)日:2012-03-23

    申请号:KR1020090126281

    申请日:2009-12-17

    Inventor: 이필호 이광무

    Abstract: 본 발명은 하기 화학식 1로 표시되는 인돌리진(indolizine) 유도체와 이의 제조방법에 관한 것이다. 보다 상세하게는, 팔라듐 촉매 존재 하 유기인듐 시약과 피리딘 유도체의 교차짝지움 반응 및 분자내 고리화 반응을 통해 상기 신규한 인돌리진(indolizine) 유도체를 제조하는 방법에 관한 것이다.
    [화학식 1]

    [상기 화학식 1에서 R 및 R
    1 내지 R
    5 는 각각 발명의 상세한 설명에서 정의한 바와 같다.]
    에틸 4-브로모-2-펜틴오에이트, 에틸 4-브로모-2-펜틴오에이트 유도체, 팔라듐, 인듐, 교차짝지움 반응, 유기인듐 시약, 분자내 고리화반응, 2-아이오도피리딘, 2-아이오도피리딘 유도체, 2-피리딜트리플루오로메탄설포네이트, 2-피리딜트리플루오로메탄설포네이트 유도체, 인돌리진 유도체

    신규한 인돌리진 유도체와 이의 제조방법
    64.
    发明公开
    신규한 인돌리진 유도체와 이의 제조방법 有权
    新型吲哚啉衍生物及其制备方法

    公开(公告)号:KR1020110069520A

    公开(公告)日:2011-06-23

    申请号:KR1020090126281

    申请日:2009-12-17

    Inventor: 이필호 이광무

    Abstract: PURPOSE: An indolizine derivative and a method for preparing the same are provided to develop novel drugs and to obtain indolizine derivative with high yield. CONSTITUTION: An indolizine derivative is denoted by chemical formula 1. In chemical formula 1, R is (C1-C7)alkyl; R1 is (C1-C7)alkyl or (C6-C20)aryl(C1-C7)alkyl; R2 is hydrogen or (C1-C7)alkyl; R3 is hydrogen, (C1-C7)alkyl, nitro, or halogen; and R4 and R5 are independently hydrogen or (C1-C7)alkyl. A method for preparing the indolizine derivative comprises a step of reacting pyridine derivatives of chemical formula 4 with organic indium reagent of chemical formula 3 under the presence of palladium catalyst and phospine ligand.

    Abstract translation: 目的:提供中和衍生物及其制备方法,以开发新型药物,并以高产率获得中氮茚衍生物。 构成:中和衍生物由化学式1表示。在化学式1中,R为(C 1 -C 7)烷基; R1是(C1-C7)烷基或(C6-C20)芳基(C1-C7)烷基; R2是氢或(C1-C7)烷基; R3是氢,(C1-C7)烷基,硝基或卤素; 且R 4和R 5独立地为氢或(C 1 -C 7)烷基。 制备中氮茚衍生物的方法包括使化学式4的吡啶衍生物与化学式3的有机铟试剂在钯催化剂和膦配体的存在下反应的步骤。

    신규한 다치환 피롤 유도체와 이의 제조방법
    65.
    发明授权
    신규한 다치환 피롤 유도체와 이의 제조방법 失效
    新型多取代吡咯衍生物及其制备方法

    公开(公告)号:KR100998556B1

    公开(公告)日:2010-12-07

    申请号:KR1020100032171

    申请日:2010-04-08

    Abstract: PURPOSE: A novel multi-substituted pyrrole derivative using organic sulfur-indium complex and a method for preparing the same are provided to use for synthesis of natural substances with pharmaceutical or physiological activity. CONSTITUTION: A multi-substituted pyrrole derivative is denoted by chemical formula 1. The multi-substituted pyrrole derivative of chemical formula 1 is prepared by performing cross coupling and intramolecular cycling of indium tri(organothiolate) of chemical formula 2(In(SR^4)_3) and tertiary propagyl with imidoyl group of chemical formula 3 under the presence of palladium catalyst and phosphine ligand or additive.

    Abstract translation: 目的:提供一种使用有机硫 - 铟络合物的新型多取代吡咯衍生物及其制备方法,用于合成具有药物或生理活性的天然物质。 组成:化学式1表示多取代吡咯衍生物。化学式1的多取代吡咯衍生物通过进行化学式2(In(SR 4))的三(有机硫酸盐)的交叉偶联和分子内循环来制备 )_3),并且在钯催化剂和膦配体或添加剂的存在下,与化学式3的亚氨基进行叔三级扩链。

    아세틸렌 유도체의 제조 방법
    66.
    发明公开
    아세틸렌 유도체의 제조 방법 有权
    乙酰衍生物的制备方法

    公开(公告)号:KR1020100104803A

    公开(公告)日:2010-09-29

    申请号:KR1020090023447

    申请日:2009-03-19

    CPC classification number: C07C67/343 C07C1/325 C07C15/54 C07C15/60 C07C69/76

    Abstract: PURPOSE: A producing method of an acetylene derivative is provided to easily produce a metal-acetylide nucleophile using a decarboxylation reaction from a propiolic acid derivative without using large amount of bases. CONSTITUTION: A producing method of an acetylene derivative marked with chemical formula 1 comprises the following steps: forming organic silver salt marked with chemical formula 4, by reacting silver salt marked with chemical formula 3 and a propiolic acid derivative marked with chemical formula 2; and reacting the organic silver salt with a compound containing palladium salt, a phosphine group ligand, and an organic halide compound marked with chemical formula 5.

    Abstract translation: 目的:提供乙炔衍生物的制备方法,使用来自丙炔酸衍生物的脱羧反应容易地生成金属 - 乙炔基亲核试剂,而不需要大量的碱。 构成:用化学式1表示的乙炔衍生物的制造方法包括以下步骤:通过使化学式3标记的银盐与化学式2所示的丙炔酸衍生物反应,形成用化学式4表示的有机银盐; 并使有机银盐与含有钯盐,膦基配位体和化学式5标记的有机卤化物的化合物反应。

    신규한 쿠마린 유도체와 이의 제조방법
    67.
    发明公开
    신규한 쿠마린 유도체와 이의 제조방법 有权
    新型香豆素衍生物及其制备方法

    公开(公告)号:KR1020100102457A

    公开(公告)日:2010-09-24

    申请号:KR1020090020852

    申请日:2009-03-11

    Inventor: 이필호 김선대

    Abstract: PURPOSE: A novel coumarin derivative and a method for preparing the same are provided to use as an important intermediate and to obtain coumarin derivative of high yield. CONSTITUTION: A novel coumarin derivative is denoted by chemical formula 1. The coumarin derivative is prepared by reacting allenoate compound of chemical formula 2 with dihydroxy benzene derivative compound, dihydroxybenzene, alkoxy benzene derivative, or alkoxy benzene of chemical formula 3 under the presence of acid. The acid is acetic acid, trifluoroacetic acid, paratoluene sulfonic acid, trifluoromethansulfonic acid or mixture thereof. The reaction is performed under the presence of dichloroethane solvent at 80-120°C.

    Abstract translation: 目的:提供一种新型香豆素衍生物及其制备方法,用作重要的中间体并获得高产率的香豆素衍生物。 构成:化学式1表示新型香豆素衍生物。香豆素衍生物通过化学式2的异烯酸酯化合物与化学式3的二羟基苯衍生物,二羟基苯,烷氧基苯衍生物或烷氧基苯在酸存在下反应制备 。 酸是乙酸,三氟乙酸,对甲苯磺酸,三氟甲磺酸或其混合物。 反应在二氯乙烷溶剂存在下在80-120℃下进行。

    신규한 알레닐 설파이드 유도체와 이의 제조방법
    68.
    发明公开
    신규한 알레닐 설파이드 유도체와 이의 제조방법 失效
    新型烯丙基化合物及其合成

    公开(公告)号:KR1020100078939A

    公开(公告)日:2010-07-08

    申请号:KR1020080137331

    申请日:2008-12-30

    Inventor: 이필호 류태규

    Abstract: PURPOSE: An allenyl sulfide derivative and a manufacturing method thereof are provided to obtain the allenyl sulfide derivative with the high yield over 70% with a simple reaction. CONSTITUTION: An allenyl sulfide derivative is marked with chemical formula 1. In the chemical formula 1, R1 and R2 are a C1~C10 alkyl group, or a C6~C12 aryl group, respectively. The R1 and the R2 are capable of forming a 3-8-membered ring by being bonded with a C2~C7 alkylene group. R3 is either the C1~C10 alkyl group, or the C6~C12 aryl group. R4 is hydrogen or the C1~C10 alkyl group.

    Abstract translation: 目的:提供烯丙基硫醚衍生物及其制备方法,以简单的反应获得70%以上的高收率的烯丙基硫醚衍生物。 结构式:烯化硫化物衍生物用化学式1表示。在化学式1中,R1和R2分别为C1〜C10烷基或C6〜C12芳基。 R1和R2能够通过与C 2〜C 7亚烷基结合形成3-8元环。 R3是C1〜C10烷基或C6〜C12芳基。 R4是氢或C1〜C10烷基。

    설파이드 화합물 및 유기 황-인듐 착물을 이용한설파이드화합물 제조방법
    69.
    发明授权

    公开(公告)号:KR100940338B1

    公开(公告)日:2010-02-04

    申请号:KR1020070122293

    申请日:2007-11-28

    Inventor: 이필호 이재영

    Abstract: 본 발명은 설파이드 화합물 및 유기 황-인듐 착물을 이용한 설파이드화합물 제조방법에 관한 것으로, 더 상세하게는 종래 합성법은 친핵체와 친전자체간의 반응으로 전이금속 촉매 반응조건에서 탄소-황 결합을 형성시켜 왔으며, 유기 헬라이드 화합물을 친전자체로 유기 티오(황) 알코올을 친핵체로 사용하여 반응을 수행하였다. 유기 티오 알코올의 낮은 친핵성을 높이기 위해 염기를 사용하여 유기 황 음이온으로 변환시켜 반응을 수행시켰으며 좀 더 높은 반응성을 위해 높은 반응 온도와 긴 반응시간이 필요로 하고 있다. 이에 본 발명은 반응에서 티오 알코올의 친핵성을 증가시키기 위해 새로운 형태의 반응시약을 반응에 응용하여 좀 더 짧은 반응시간에 높은 반응 수율을 갖는 반응을 개발하며, 나아가 개발한 반응의 유용성을 보여주기 위해 종래에 합성법이 알려지지 않았거나 합성에 어려움이 있는 설파이드 화합물을 합성하고 기질내 친전자성을 띄는 부분이 2개 이상인 경우에도 시약을 과량으로 사용하지 않아도 정량적인 반응이 일어나는 효과적이며 새로운 합성법을 제공하는 설파이드 화합물의 합성방법에 관한 것이다.
    설파이드 화합물, 설파이드 화합물 합성, 팔라듐, 유기황-인듐, 교차-짝지움 반응

    인아인-1,6-다이올 화합물과 이의 제조방법
    70.
    发明公开
    인아인-1,6-다이올 화합물과 이의 제조방법 失效
    ENYNE-1,6-DIOL衍生物及其合成

    公开(公告)号:KR1020090131048A

    公开(公告)日:2009-12-28

    申请号:KR1020080056823

    申请日:2008-06-17

    Abstract: PURPOSE: A method for manufacturing enyne-1,6-diol derivatives is provided to selectively synthesize enyne-1,6-diol derivatives by reacting an allyl indium reagent with an allenyn-1,6-diol compound through in-situ reaction without separate refining process. CONSTITUTION: A method for manufacturing enyne-1,6-diol derivatives comprises the steps of: reacting an allyl halide derivative represented by chemical formula 3 and indium to prepare an allyl indium reagent represented by chemical formula 4; and reacting an allylnyne-1,6-diol compound represented by chemical formula 2 to prepare an enyne-1,6-diol derivative represented by chemical formula 1.

    Abstract translation: 目的:提供一种制备烯-1,6-二醇衍生物的方法,通过原位反应使烯丙基铟试剂与全烯-1,6-二醇化合物反应而选择性合成烯-1,6-二醇衍生物,无需分离 精炼过程。 构成:制造烯-1,6-二醇衍生物的方法包括以下步骤:使由化学式3表示的烯丙基卤化物衍生物与铟反应,制备由化学式4表示的烯丙基铟试剂; 并使由化学式2表示的烯丙基-1,6-二醇化合物反应,制备由化学式1表示的烯-1,6-二醇衍生物。

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