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    9-oximesilyl erythromycin a derivative
    2.
    发明专利
    9-oximesilyl erythromycin a derivative 审中-公开
    9-OXIMESILYL ERYTHROMYCIN A DERIVATIVE

    公开(公告)号：JP2007224035A

    公开(公告)日：2007-09-06

    申请号：JP2007100369

    申请日：2007-04-06

    Applicant: Abbott Lab ,  アボット・ラボラトリーズAbbott Laboratories

    Inventor： KU YI-YIN

    IPC: C07H17/08 ,  A61K31/7048

    CPC classification number: C07H17/08

    Abstract: PROBLEM TO BE SOLVED: To provide a quick and efficient method for producing 6-O-alkylerythromycin A by using a moderate and neutral reaction condition for suppressing the formation of undesirable byproducts. SOLUTION: This method for producing a 9-O-oximesilyl-6-O-alkyl erythromycin A derivative is provided by forming a 9-oximesilyl erythromycin A derivative by silylating a 9-oxime erythromycin A derivative, then reacting the 9-oximesilyl erythromycin A derivative with an alkylating agent and selectively alkylating at 6-oxygen. Further, the method for producing the 6-O-alkyl erythromycin A comprises the deoximation of the 9-O-oximesilyl-6-O-alkyl erythromycin A derivative. The 6-O-alkyl erythromycin A produced by the above method, e.g. clarythromycin is an important macrolide-based antibiotic. COPYRIGHT: (C)2007,JPO&INPIT

    Abstract translation: 待解决的问题：提供一种通过使用中等和中性反应条件来抑制不期望的副产物的形成来快速有效地生产6-O-烷基红霉素A的方法。 解决方案：通过将9-肟基红霉素A衍生物甲硅烷基化，然后使9-肟基红霉素A衍生物与9-肟基红霉素A衍生物反应， 肟基红霉素A衍生物与烷基化剂并在6-氧选择性烷基化。 此外，制备6-O-烷基红霉素A的方法包括9-O-肟基-6-O-烷基红霉素A衍生物的脱肟。 通过上述方法制备的6-O-烷基红霉素A，例如 氯霉素是一种重要的大环内酯类抗生素。 版权所有（C）2007，JPO＆INPIT

    PROCESS FOR PREPARING AMINE TYPE SUBSTITUTED BENZOFURANS
    6.
    发明申请
    PROCESS FOR PREPARING AMINE TYPE SUBSTITUTED BENZOFURANS 审中-公开
    制备胺类替代苯并呋喃的方法

    公开(公告)号：WO2004024707A3

    公开(公告)日：2004-08-12

    申请号：PCT/US0328396

    申请日：2003-09-10

    Applicant: ABBOTT LAB

    Inventor： KU YI-YIN ,  PU YU-MING ,  COWART MARLON D ,  GRIEME TIMOTHY A ,  GUPTA ASHOK K ,  PLATA DANIEL J

    IPC: C07C253/30 ,  C07C255/53 ,  C07D307/81 ,  C07D405/04 ,  C07C15/14 ,  C07D307/80 ,  C07D407/04

    CPC classification number: C07D405/04 ,  C07C253/30 ,  C07C255/53 ,  C07D307/81

    Abstract: The present invention relates to processes for preparing amine substituted benzofurans, and more particularly 4-(2-{2-[(2R)-2-methyl-1-pyrrolidinyl]ethyl}-1-benzofuran-5-yl)benzonitrile, and salts thereof. Compounds prepared by the processes of the invention have demonstrated activity as histamine-3 receptor ligands. Forumla (I) or a salt thereof, wherein A is heterocycle selected from pyrrolidinyl or piperidinyl, wherein he heterocycle is substituted with 0, 1, 2, 3 or 4 substituents selected from the group consisting of alkyl and fluoroalkyl; and R 1 is 4-cyanophenyl, aryl, or heteroaryl, wherein he phenyl of 4-cyanophenyl, the aryl, or the heteroaryl is substituted with 0, 1, 2, 3 or 4 substituents seleced from the group consisting of alkoxy, alkoxyalkyl, alkyl, alkylthio, alkylthioalkyl, cyano, haloalkoxy, halogen, and haloalkyl.

    Abstract translation: 本发明涉及制备胺取代的苯并呋喃的方法，特别是4-（2- {2 - [（2R）-2-甲基-1-吡咯烷基]乙基} -1-苯并呋喃-5-基）苄腈，和 的盐。 通过本发明方法制备的化合物已经证明作为组胺-3受体配体的活性。 （I）化合物或其盐，其中A是选自吡咯烷基或哌啶基的杂环，其中杂环被0,1,2,3或4个选自烷基和氟代烷基的取代基取代; 并且R 1是4-氰基苯基，芳基或杂芳基，其中4-氰基苯基，芳基或杂芳基的苯基被0,1,2,3或4个取代基取代，所述取代基选自烷氧基，烷氧基烷基， 烷基，烷硫基，烷硫基烷基，氰基，卤代烷氧基，卤素和卤代烷基。

    METHOD FOR SEPARATION OF GIBBERELLIN MIXTURES.
    7.
    发明公开
    METHOD FOR SEPARATION OF GIBBERELLIN MIXTURES. 失效
    VERFAHREN ZUR TRENNUNG VON GIBBERELLINMISCHUNGEN。

    公开(公告)号：EP0588964A4

    公开(公告)日：1995-02-08

    申请号：EP92914330

    申请日：1992-06-12

    Applicant: ABBOTT LAB

    Inventor： KU YI-YIN ,  SAWICK DAVID PETER

    IPC: C07D307/935 ,  C07F7/02 ,  C07F7/18 ,  C07D307/77

    CPC classification number: C07D307/935 ,  C07F7/1856

    Abstract: A method for the separation of gibberellins from mixtures thereof by selective silylation or desilylation, as well as substantially pure gibberellins prepared thereby. For example, to a solution of a mixture of GA4 and GA7 in DMF was added imidazole. After imidazole was completely dissolved, butyldimethylsilyl chloride was added. After two days of stirring, acetic acid was added which precipitated a white solid (silyl ether of GA7). After filtration GA4 was recovered from the filtrate. Desilylation of the silyl ether of GA7 yielded GA7.

    Abstract translation: 通过选择性甲硅烷基化或脱硅烷基化将赤霉素与其混合物分离的方法，以及由此制备的基本上纯的赤霉素。 例如，向GA4和GA7的混合物的DMF溶液中加入咪唑。 咪唑完全溶解后，加入丁基二甲基甲硅烷基氯。 搅拌两天后，加入乙酸，沉淀出白色固体（GA7的甲硅烷基醚）。 过滤后，从滤液中回收GA4。 GA7的甲硅烷基醚的脱甲硅烷基化得到GA7。

    9-OXIMESILYL ERYTHROMYCIN A DERIVATIVES
    8.
    发明专利
    9-OXIMESILYL ERYTHROMYCIN A DERIVATIVES 未知

    公开(公告)号：CA2250771C

    公开(公告)日：2006-05-02

    申请号：CA2250771

    申请日：1997-02-06

    Applicant: ABBOTT LAB

    Inventor： KU YI-YIN

    IPC: C07H17/08 ,  C07H23/00

    Abstract: A process of preparing 6-O-alkylerythromycin A using 9-oximesilyl erythromyc in A derivatives is provided. 9-Oximesilyl- and 6-O-alkylerythromycin A derivatives used in the preparation of 6-O- alkylerythromycin A are also provided.

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