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    옥시라세탐의 제조방법
    1.
    发明授权
    옥시라세탐의 제조방법 失效
    옥시라세탐의제조방법

    公开(公告)号：KR100424393B1

    公开(公告)日：2004-03-24

    申请号：KR1020010073696

    申请日：2001-11-26

    Applicant: 한국화학연구원

    Inventor： 박태호 ,  이상호 ,  한철 ,  김선주

    IPC: C07D207/12

    Abstract: PURPOSE: A method of preparing oxiracetam is provided to make oxiracetam product in high purity and yield. The oxiracetam improves brain functions and therapeutic effect on dementia. CONSTITUTION: In a method of preparing oxiracetam of the formula(1), a tri-amide compound of the formula(2) is first prepared by reacting an organic solvent compound of the formula(4) with an organic solvent compound of the formula(5). A compound of the formula(3) is prepared by sequentially conducting cyclization, decarboxylation and reduction with respect to the compound of the formula(2). The compound of the formula(3) reacts with ammonia under the existence of water or alcohol. In the formulae, R is methyl group or ethyl group, and X is hydroxy group or halide. The cyclization of the compound of the formula(2) is achieved by reaction with hydride or alkoxide at -30-50 deg.C for 1-15 hours.

    Abstract translation: 目的：提供制备奥拉西坦的方法以制备高纯度奥拉西坦产物。 奥拉西坦改善脑功能和对痴呆的治疗效果。 构成：在制备式（1）的奥拉西坦的方法中，式（2）的三酰胺化合物首先通过使式（4）的有机溶剂化合物与式（2）的有机溶剂化合物 5）。 式（3）的化合物通过对式（2）的化合物依次进行环化，脱羧和还原来制备。 式（3）的化合物在水或醇存在下与氨反应。 式中，R为甲基或乙基，X为羟基或卤素。 式（2）化合物的环化通过在-30-50℃下与氢化物或醇盐反应1-15小时来实现。

    3-메톡시이미노-4-아미노메틸피롤리딘 유도체의 제조방법
    2.
    发明公开
    3-메톡시이미노-4-아미노메틸피롤리딘 유도체의 제조방법 失效
    制备3-甲氧基亚氨基-4-氨基甲基吡咯烷衍生物的方法

    公开(公告)号：KR1020020003786A

    公开(公告)日：2002-01-15

    申请号：KR1020000038153

    申请日：2000-07-05

    Applicant: 한국화학연구원

    Inventor： 박태호 ,  이상호 ,  한철 ,  김선주 ,  성길연 ,  곽형섭

    IPC: C07D207/22

    Abstract: PURPOSE: Provided is a method for preparing 3-methoxyimino-4-aminomethylpyrrolidine derivatives, which are used as a useful substituent for the position No.7 of quinolone antibiotics, from 1-benzyl-3-oxo-4-ethoxycarbo0nylpyrrolidine. CONSTITUTION: The method comprises the steps of: reacting a compound of the formula(2) with oxoamine compound or its salt to prepare a compound of the formula(3); reducing a compound of the formula(3) to prepare a compound of the formula(4); hydrogenating and amine-protecting the compound of the formula(4) to prepare a compound of the formula(5); sulfonating the compound of the formula(5) to prepare a compound of the formula(6); aminating or azidonating the compound of the formula(6) to prepare a compound of the formula(8a) or a compound of the formula(7) respectively; hydrogenating the compound of the formula(7) to prepare a compound of the formula(8a) or reacting the compound of the formula(6) with amide to prepare a compound of the formula(8b); and reacting the compound of the formula(8a) or (8b) with acid to deprotect amine.

    Abstract translation: 目的：提供3-甲氧基亚氨基-4-氨基甲基吡咯烷衍生物作为喹诺酮类抗生素的第7位的有用取代基，由1-苄基-3-氧代-4-乙氧基羰基吡咯烷制备的方法。 方法：该方法包括以下步骤：使式（2）的化合物与氧代胺化合物或其盐反应以制备式（3）的化合物; 还原式（3）的化合物以制备式（4）的化合物; 氢化和胺保护式（4）化合物以制备式（5）化合物; 磺化式（5）化合物以制备式（6）化合物; 胺化或叠氮化式（6）化合物以分别制备式（8a）化合物或式（7）化合物; 氢化式（7）的化合物以制备式（8a）的化合物或使式（6）的化合物与酰胺反应以制备式（8b）的化合物; 并使式（8a）或（8b）的化合物与酸反应以使胺脱保护。

    신규한 벤조피란계 히드록시메틸화 대사산물 및 유도체
    6.
    发明授权
    신규한 벤조피란계 히드록시메틸화 대사산물 및 유도체 失效
    新型苯并吡喃类羟甲基化代谢物和衍生物

    公开(公告)号：KR1019960015006B1

    公开(公告)日：1996-10-23

    申请号：KR1019930008366

    申请日：1993-05-15

    Applicant: 한국화학연구원

    Inventor： 유성은 ,  서지희 ,  김선주

    IPC: C07D405/04

    Abstract: This invention relates to the pharmaceutical composite containing benzopyran group hydroxylmethyl metabolite or its derivatives useful to reduce blood pressure wherein the benzopyran derivatives having following formula(I). In the formula, R1 is -CN, -NO2, OCX1X2X3, NH2, -NHSO2Ra, -NHCORb, -CONRcRd, -SO2Rc or -SO2NRcRd wherein X1, X2 and X3 are separate F, Cl or H; Ra and Rb are separate amino, C1-6 alkoxyl, C1-6 alkyl or phenyl; Rc and Rd are separate halogen, C1-6 alkyl or replaced/or not replaced phenyl; R2 is like the formula where Re is C1-6 alkyl, cyclopropyl, cyclopropyl methyl or benzyl; Rf is -CORa or -CSRa, X is O, S or NRc, and Y is H, C1-6 linear or side chain alkyl, halogen, amino or C16 alkoxy, and n is between 0 and 3; R3 is replaced or not replaced C1-4 linear or side chain alkyl.

    Abstract translation: 本发明涉及含有苯并吡喃基羟甲基代谢物或其衍生物的药物复合物，其用于降低血压，其中具有下式（I）的苯并吡喃衍生物。 式中，R1为-CN，-NO2，OCX1X2X3，NH2，-NHSO2Ra，-NHCORb，-CONRcRd，-SO2Rc或-SO2NRcRd，其中X1，X2和X3分别为F，Cl或H; R a和R b分别是氨基，C 1-6烷氧基，C 1-6烷基或苯基; Rc和R d分别是卤素，C 1-6烷基或被取代的或未被取代的苯基; R 2如下式，其中Re为C 1-6烷基，环丙基，环丙基甲基或苄基; Rf为-CORa或-CSRa，X为O，S或NRc，Y为H，C1-6直链或侧链烷基，卤素，氨基或C16烷氧基，n为0至3; R3被取代或未被C 1-4直链或侧链烷基取代。

    벤조피란 유도체와 그의 제조방법
    8.
    发明授权
    벤조피란 유도체와 그의 제조방법 失效
    苯并吡喃衍生物及其制备方法

    公开(公告)号：KR1019950009863B1

    公开(公告)日：1995-08-29

    申请号：KR1019910024353

    申请日：1991-12-26

    Applicant: 한국화학연구원

    Inventor： 유성은 ,  정낙철 ,  서지희 ,  김선주

    IPC: C07D405/04

    CPC classification number: C07D405/04 ,  C07D405/14

    Abstract: The cpd. of formula (I-a) is prepd. by (a) reacting ketone derivatives of formula (II) with trifluorosulfonic acid anhydride and ter-amine, or making the ketone derivatives (II) to enolate with a base and then reacting N-phenyl trifluoromethane sulfonimide to convert to the vinyl triflate derivs. of formula (III); and (b) reacting the derivs. (III) with trialkyline derivs. of formula (IV). In the formulas, R1 is -CN, -NO2, -OCX1X2X3 or -SO2Rc; X1, X2, and X3 are F, Cl or H(however, X1=X2=X3=H); R2 is straight or branched C1-4 alkyl; R3 is straight or branched C1-4 alkyl, etc; R4 is C1-4 alkyl.

    Abstract translation: cpd。 的式（I-a）是制备的。 通过（a）使式（II）的酮衍生物与三氟磺酸酐和三胺反应，或使酮衍生物（II）与碱烯醇化，然后使N-苯基三氟甲磺酰亚胺反应转化成三氟甲磺酸乙烯酯衍生物。 的式（III）; 和（b）使衍生物反应。 （III）与三烷基衍生物。 的式（IV）化合物。 式中，R 1为-CN，-NO 2，-OCX 1 X 2 X 3或-SO 2 R c; X1，X2和X3分别为F，Cl或H（但X1 = X2 = X3 = H）; R2是直链或支链C 1-4烷基; R3是直链或支链C 1-4烷基等; R4是C1-4烷基。

    벤조피란 유도체와 그의 제조방법(1)
    9.
    发明授权
    벤조피란 유도체와 그의 제조방법(1) 失效
    苯并吡喃衍生物及其制备方法

    公开(公告)号：KR1019950009862B1

    公开(公告)日：1995-08-29

    申请号：KR1019910024352

    申请日：1991-12-26

    Applicant: 한국화학연구원

    Inventor： 유성은 ,  이규양 ,  정낙철 ,  서지희 ,  김선주 ,  신화섭 ,  이병호 ,  정규식

    IPC: C07D405/04

    CPC classification number: C07D405/04 ,  C07D405/14

    Abstract: Benzopyran derivatives of formula (I) are prepd. by (a) reacting the epoxy cpd. of formula (II) with a nucleophilic agent contg. cpd. to prepare the alcohol dervs. of formula (III), in the presence of a base; (b) dehydration reacting the cpd. (III) in the presence of a base. In the formulas, R1 is -CN, -NO2, OCX1X2X3 or -SO2Rc; X1, X2 and X3 are eachly F, Cl or H; Rc is H, C1-6 alkyl or opt. satd. phenyl where satd. gp. is halogen, or straight or branched C1-3 alkyl. The obptd. benzopyran dervs. are useful for curing hypertension.

    Abstract translation: 式（I）的苯并吡喃衍生物是制备的。 通过（a）使环氧树脂cpd反应。 的式（II）与亲核剂 CPD。 准备酒精dervs。 在式（III）的存在下， （b）使cpd反应脱水。 （III）在碱的存在下。 式中，R 1为-CN，-NO 2，OCX 1 X 2 X 3或-SO 2 R c; X1，X2和X3分别为F，Cl或H; Rc是H，C 1-6烷基或选择。 饱和。 苯基，其中satd GP。 是卤素，或直链或支链C 1-3烷基。 绝对的 苯并吡喃衍生物 可用于治疗高血压。

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