레복세틴 부분입체이성질체 유도체의 신규한 제조방법
    21.
    发明授权
    레복세틴 부분입체이성질체 유도체의 신규한 제조방법 有权
    制备瑞波西汀非对映异构体衍生物的新方法

    公开(公告)号:KR101432726B1

    公开(公告)日:2014-08-22

    申请号:KR1020110147494

    申请日:2011-12-30

    Abstract: 본 발명은 레복세틴 부분입체이성질체 유도체의 신규한 제조방법에 관한 것이다. 본 발명에 의한 제조방법으로 제조된 레복세틴 부분입체이성질체 유도체는 수율이 매우 우수하고, 제조과정이 간단할 뿐만 아니라, 특히, 하이드록시기가 보호된 신나밀알코올에 비대칭 다이히드록시화 반응을 수행함으로써, 산소 작용기를 입체선택적으로 도입한 후, 상기 다이올(diol)을 사이클릭 설페이트의 형태로 변형시킨 후, 상기 다이올을 동시에 활성화하며, 보호기로 보호된 하이드록시기의 탈보호 과정으로 유발되는 사이클릭 설페이트 재배열반응(cyclic sulfate rearrangement)이 일어남으로써, 친핵성 치환반응이 가능해지고, 이때, 지금까지 보고되지 않은 신규의 에폭시 생성반응이 동반될 뿐만 아니라, 이 과정에서 다른 워크업 과정없이 동일 반응용기(one pot)에서 다음반응을 수행할 수 있어 반응 단계가 줄어들어 합성시간이 짧아 매우 효율적으로 레복세틴 부분입체이성질체 유도체를 제조할 수 있고, 또한, 레복세틴은 세로토닌 노르에피네프린 재흡수 억제 효과가 있으므로 이의 부분입체이성질체인 본 발명에 따른 레복세틴 부분입체이성질체 유도체는 우울증 및 주의력 결핍 및 과잉행동장애(ADHD) 예방 또는 치료용 약학적 조성물로 유용하게 사용될 수 있다.

    신규한 자일로시다아제 KRICT PX D4
    22.
    发明公开
    신규한 자일로시다아제 KRICT PX D4 有权
    新颖的B-D-XYLOSIDASES具有XYLOLYTIC活性的KRICT PXD4

    公开(公告)号:KR1020140015042A

    公开(公告)日:2014-02-06

    申请号:KR1020120082713

    申请日:2012-07-27

    Abstract: The present invention provides xylosidase having amino acid sequence described in second sequence in a sequence listing. More specifically, the xylosidase of the present invention has heat resistance and alkali resistance. The xylosidase reduces wastes and expensive purification costs by replacing conventional chemical methods, and can be used for manufacturing raw materials such as substitute raw materials for fuel, special functional materials, bio polymers, and the likes by being utilized in a saccharification process of fiber based biomass, in forage industries, and paper and detergent industries by showing excellent xylene decomposition activities.

    Abstract translation: 本发明提供了序列表中具有第二序列描述的氨基酸序列的木糖苷酶。 更具体地说,本发明的木糖苷酶具有耐热性和耐碱性。 木糖苷酶通过替代常规的化学方法减少了废物和昂贵的净化成本,并且可以用于制造诸如燃料替代原料,特殊功能材料,生物聚合物等原料,用于纤维基的糖化过程 生物质,饲料工业,造纸和洗涤剂行业,显示出优异的二甲苯分解活性。

    바이오매스로부터 셀룰로오스 유도체의 제조방법
    23.
    发明公开
    바이오매스로부터 셀룰로오스 유도체의 제조방법 无效
    从生物量制备纤维素衍生物的方法

    公开(公告)号:KR1020130125724A

    公开(公告)日:2013-11-19

    申请号:KR1020130051208

    申请日:2013-05-07

    CPC classification number: C08B15/00 C08B1/00

    Abstract: The present invention relates to a method for preparing cellulose derivatives from biomass comprising the following steps: treating room temperature ionic liquid with biomass including cellulose, hemi-cellulose and lignin, and dissolving the cellulose; removing the room temperature ionic liquid and recrystallizing the cellulose; and making a functional-group-introducing agent to contact with the recrystallized cellulose, and introducing a functional group to the cellulose in order to obtain cellulose derivatives. The present invention excludes effects of foreign substances and excessive decomposition products generated in existing pre-processing steps, reduces costs, prevents environmental contamination by simplifying processes and recycling the room temperature ionic liquid, concurrently obtains various cellulose derivatives and saves energy consumed for pre-processing by processing the steps at the room temperature.

    Abstract translation: 本发明涉及从生物质制备纤维素衍生物的方法,包括以下步骤:用包括纤维素,半纤维素和木质素在内的生物质处理室温离子液体,并溶解纤维素; 去除室温离子液体并重结晶纤维素; 并且使官能团引入剂与再结晶纤维素接触,并将官能团引入纤维素以获得纤维素衍生物。 本发明不包括在现有预处理步骤中产生的异物和过量分解产物的影响,降低成本,通过简化工艺和回收室温离子液体来防止环境污染,同时获得各种纤维素衍生物并节省预处理所消耗的能量 通过在室温下处理步骤。

    [1,2,3]-옥사티아졸리딘-2,2-디옥사이드 또는 [1,2,5]-티아디아졸리딘-1,1-디옥사이드 유도체의 제조방법
    24.
    发明公开
    [1,2,3]-옥사티아졸리딘-2,2-디옥사이드 또는 [1,2,5]-티아디아졸리딘-1,1-디옥사이드 유도체의 제조방법 有权
    制备[1,2,3] - 氧杂环丁烷-2,2-二氧化物或[1,2,5] - 二氮杂环丁烷-1,1-二氧化物衍生物的方法

    公开(公告)号:KR1020110138600A

    公开(公告)日:2011-12-28

    申请号:KR1020100058586

    申请日:2010-06-21

    CPC classification number: C07D285/10 C07D291/04 C07D419/04

    Abstract: PURPOSE: A method for preparing [1,2,3]-oxathiazolidine-2,2-dioxide or derivative thereof is provided to simply and efficiently obtain the enantiomerically pure compounds. CONSTITUTION: A method for preparing a compound of chemical formula 1a or 1b with optical activity comprises a step of performing asymmetric reduction of a compound of chemical formula 2 under the presence of a hydrogen donor and a rhodium compound catalyst containing pentamethylcyclopentadienyl group. The hydrogen donor is formic acid, metal salt thereof of. The compound of chemical formula 2 is prepared by reacting alpha-hydroxy ketone of chemical formula 4 with sulfamide of chemical formula 5 by thermal reflux or under an acidic condition.

    Abstract translation: 目的:提供制备[1,2,3] - 氧杂噻唑烷-2,2-二氧化物或其衍生物的方法简单有效地获得对映体纯的化合物。 构成:具有光学活性的化学式1a或1b化合物的制备方法包括在氢供体和含有五甲基环戊二烯基的铑化合物催化剂的存在下进行化学式2的化合物的不对称还原的步骤。 氢供体是甲酸,其金属盐。 化学式2的化合物通过使化学式4的α-羟基酮与化学式5的磺酰胺通过热回流或在酸性条件下反应来制备。

    광학 활성 2-설포닐옥시-1-헤테로아릴에탄올 유도체의 제조방법 및 이를 이용한 거울상 이성질체적으로 순수한 부푸랄롤의 제조방법

    公开(公告)号:KR1020110006377A

    公开(公告)日:2011-01-20

    申请号:KR1020090063981

    申请日:2009-07-14

    Inventor: 이기인 곽세훈

    Abstract: PURPOSE: A method for preparing optically active 2-sulfonyl oxy-1-heteroaryl ethanol derivative is provided to prepare pure bufuralol of optical isomer. CONSTITUTION: A 2-sulfony oxy-1-heteroaryl ethanol derivative is prepared by asymmetric reduction of alpha-sulfonyl oxy hetero aryl ketone compound of chemical formula 3 under the presence of hydrogen donor and rhodium compound catalyst containing pentamethyl cyclopentadienyl group of chemical formula 4. The hydrogen donor is formic acid or metal salt or ammonium salt thereof. The hydrogen donor is used without a solvent or is dissolved in a solvent. The solvent is ethyl acetate, toluene, methylene chloride, dimethylform amide(DMF), tetrahydrofurane(THF), acetonitrile or isopropanol. A pure bufuralol is prepared by reacting the optically active 2-sulfonyl oxy-1-heteroaryl ethanol derivative compound of chemical formula 1c or 1d with t-butyl amine.

    Abstract translation: 目的:提供光学活性2-磺酰基氧基-1-杂芳基乙醇衍生物的制备方法,以制备光学异构体的纯糠醛醇。 组成:2-磺基氧基-1-杂芳基乙醇衍生物是通过化学式3的α-磺酰氧基杂芳基酮化合物在含氢化合物4的五甲基环戊二烯基的氢供体和铑化合物催化剂的存在下不对称还原制备的。 氢供体是甲酸或其金属盐或铵盐。 氢供体无溶剂使用或溶解于溶剂中。 溶剂为乙酸乙酯,甲苯,二氯甲烷,二甲基甲酰胺(DMF),四氢呋喃(THF),乙腈或异丙醇。 通过使化学式1c或1d的光学活性2-磺酰基氧基-1-杂芳基乙醇衍生物化合物与叔丁基胺反应来制备纯糠醛。

    이염화 이소사이아니드를 이용한 옥사졸리딘-2-온 화합물의제조방법
    27.
    发明公开
    이염화 이소사이아니드를 이용한 옥사졸리딘-2-온 화합물의제조방법 有权
    通过使用异氰酸酯二氯化物制备氧杂环丁烷-2-酮的方法

    公开(公告)号:KR1020090124620A

    公开(公告)日:2009-12-03

    申请号:KR1020080050937

    申请日:2008-05-30

    Abstract: PURPOSE: A method of preparing oxazolidine-2-one compound is provided to apply in industry through single process with same reaction group. CONSTITUTION: A method for preparing an oxazolidin-2-one compound comprises: a step of reacting diol initiator with isocyanide dichloride to prepare cyclic iminocarbonate; and a step of performing rearrangement of the cyclic iminocarbonate with halogenation nucleophile to produce the oxazolidin-2-one function group.

    Abstract translation: 目的:提供制备恶唑烷-2-酮化合物的方法,通过单一工艺与工业上相同的反应组合使用。 构成:制备恶唑烷-2-酮化合物的方法包括:使二醇引发剂与异氰化二氯化物反应制备环状亚氨基碳酸酯的步骤; 以及用卤化亲核试剂进行环状亚氨基碳酸酯的重排以产生恶唑烷-2-酮官能团的步骤。

    아토목세틴 및 (R)-니속세틴의 제조방법
    28.
    发明公开
    아토목세틴 및 (R)-니속세틴의 제조방법 有权
    制备阿托品和(R) - 异环素的方法

    公开(公告)号:KR1020090103014A

    公开(公告)日:2009-10-01

    申请号:KR1020080028335

    申请日:2008-03-27

    Inventor: 이종철 이기인

    Abstract: PURPOSE: A method for preparing atomoxetine and (R)-nisoxetine is provided to efficiently prepare atomoxetine and (R)-nisoxetine with high optical activity through asymmetric hydrogenation transfer reaction. CONSTITUTION: A method for preparing atomoxetine and (R)-nisoxetine comprises the steps of: preparing a compound of the chemical formula 4 by reducing a compound of the chemical formula 3 through asymmetric transfer hydrogenation in the presence of a catalyst and hydrogen donor; preparing a compound of the chemical formula 5 by reacting the compound of the chemical formula 4 with a nitrile compound; preparing a compound of the chemical formula 6 by reducing the compound of the chemical formula 5 in the presence of BH3; preparing a compound of the chemical formula 7 by introducing a t-butoxycarbonyl group as a blocking group to an amine group of the compound of the chemical formula 6; prep aring a compound of the chemical formula 8 from the compound of the chemical formula 7 using Mitsunobu reaction; preparing a compound of the chemical formula 9 by introducing a methyl group to the compound of the chemical formula 8 in the presence of a base; and deprotecting the compound of the chemical formula 9 in the presence of an acid.

    Abstract translation: 目的:制备阿托西汀和(R) - 尼索西汀的方法,通过不对称氢化转移反应有效地制备具有高光学活性的阿托西汀和(R) - 尼索西汀。 构成:制备阿托莫西汀和(R) - 尼索西汀的方法包括以下步骤:通过在催化剂和氢供体的存在下通过不对称转移氢化还原化学式3的化合物来制备化学式4的化合物; 通过使化学式4的化合物与腈化合物反应制备化学式5的化合物; 通过在BH 3存在下还原化学式5的化合物来制备化学式6的化合物; 通过将化学式6的化合物的胺基引入作为封端基的叔丁氧基羰基,制备化学式7的化合物; 使用Mitsunobu反应从化学式7的化合物制备化学式8的化合物; 通过在碱存在下将化学式8的化合物引入甲基来制备化学式9的化合物; 并在酸的存在下使化学式9的化合物脱保护。

    활성 성분으로 피라졸옥심 유도체를 포함하는 항암제조성물
    29.
    发明授权
    활성 성분으로 피라졸옥심 유도체를 포함하는 항암제조성물 失效
    含有作为活性成分的吡唑氧化衍生物的抗原剂的组合物

    公开(公告)号:KR100634399B1

    公开(公告)日:2006-10-16

    申请号:KR1020040103586

    申请日:2004-12-09

    Abstract: 본 발명은 활성 성분으로서 하기 화학식 1의 피라졸옥심 유도체를 포함하는 항암제 조성물에 관한 것이다.
    본 발명의 조성물에 사용된 화학식 1의 피라졸옥심 유도체는 합성 방법이 매우 간단할 뿐 아니라, 폐암, 난소암, 흑색종, 중추신경계 종양 또는 결장암 등의 각종 암에 뛰어난 항암 활성을 보이므로, 그의 예방 및 치료에 사용될 수 있다:

    상기 식에서,
    R은, 질소함유 헤테로 고리, 치환되거나 치환되지 않은 페녹시, 페닐티오, 하이드록시, 아미노, 알킬아미노 또는 할로겐이다.

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