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    CRYSTAL FORM I OF CLARITHROMYCIN
    1.
    发明申请
    CRYSTAL FORM I OF CLARITHROMYCIN 审中-公开
    克拉霉素的晶体形式

    公开(公告)号：WO1998004573A1

    公开(公告)日：1998-02-05

    申请号：PCT/US1997013128

    申请日：1997-07-25

    Applicant: ABBOTT LABORATORIES

    Inventor： ABBOTT LABORATORIES ,  LIU, Jih-Hua ,  RILEY, David, A. ,  SPANTON, Stephen, G.

    IPC: C07H17/08

    CPC classification number: C07H17/08

    Abstract: The present invention concerns the novel antiobiotic 6-O-methylerythromycin A crystal Form I, a process for its preparation, pharmaceutical compositions comprising this compound and a method of use as a therapeutic agent.

    Abstract translation: 本发明涉及新型抗生素6-O-甲基红霉素A晶型I，其制备方法，包含该化合物的药物组合物和用作治疗剂的方法。

    IMPROVED PROCESSES FOR THE PREPARATION OF D-CHIRO-INOSITOL
    3.
    发明申请
    IMPROVED PROCESSES FOR THE PREPARATION OF D-CHIRO-INOSITOL 审中-公开
    改进D-氟尿嘧啶的制备方法

    公开(公告)号：WO1996015088A1

    公开(公告)日：1996-05-23

    申请号：PCT/US1995014437

    申请日：1995-11-09

    Applicant: ABBOTT LABORATORIES

    Inventor： ABBOTT LABORATORIES ,  RILEY, David, A. ,  BHATIA, Ashok, V. ,  CHAMBERLIN, Steven, A. ,  ROBINSON, Gregg, E.

    IPC: C07C29/10

    CPC classification number: C07C69/013 ,  C07C29/095 ,  C07C35/16

    Abstract: A method for the preparation D-chiro-inositol (I) from kasugamycin (II), comprising the steps of: (a) reacting kasugamycin with an acetylating agent to form a crude hexa-acetate intermediate; (b) purifying the crude intermediate to form purified hexa-acetate intermediate; (c) deacetylating the purified intermediate to form D-chiro-inositol; and (d) isolating the D-chiro-inositol. The method permits efficient, large-scale preparation of D-chiro-inositol without the need for extensive chromatographic purification of the final D-chiro-inositol product.

    Abstract translation: 一种从春雷霉素（II）制备D-手性肌醇（I）的方法，包括以下步骤：（a）使春雷霉素与乙酰化试剂反应以形成六醋酸中间体; （b）纯化粗中间体以形成纯化的六醋酸酯中间体; （c）将纯化的中间体脱乙酰以形成D-手性肌醇; 和（d）分离D-手性肌醇。 该方法可有效，大规模地制备D-手性肌醇，而不需要对最终D-手性肌醇产品进行广泛的色谱纯化。

    CRYSTAL FORM 0 OF CLARITHROMYCIN
    4.
    发明申请
    CRYSTAL FORM 0 OF CLARITHROMYCIN 审中-公开
    克拉霉素的晶体形式0

    公开(公告)号：WO1998031699A1

    公开(公告)日：1998-07-23

    申请号：PCT/US1997023607

    申请日：1997-12-19

    Applicant: ABBOTT LABORATORIES

    Inventor： ABBOTT LABORATORIES ,  SPANTON, Stephen, G. ,  HENRY, Rodger, F. ,  RILEY, David, A. ,  LIU, Jih-Hua

    IPC: C07H17/08

    CPC classification number: C07H17/08

    Abstract: The present invention concerns the novel antibiotic 6-O-methylerythromycin A form 0 solvate of formula (I), a process for its preparation, pharmaceutical compositions comprising this compound and a method of use as a therapeutic agent.

    Abstract translation: 本发明涉及式（I）的新型抗生素6-O-甲基红霉素A型0溶剂合物，其制备方法，包含该化合物的药物组合物和用作治疗剂的方法。

    PROCESS FOR PREPARATION OF 4-DEOXYERYTHROMYCINS A AND B
    5.
    发明申请
    PROCESS FOR PREPARATION OF 4-DEOXYERYTHROMYCINS A AND B 审中-公开
    制备4-去氧肉桂素A和B的方法

    公开(公告)号：WO1998031698A1

    公开(公告)日：1998-07-23

    申请号：PCT/US1997023356

    申请日：1997-12-18

    Applicant: ABBOTT LABORATORIES

    Inventor： ABBOTT LABORATORIES ,  PAREKH, Shyamal, I. ,  GRAHAM, Alexandra, E. ,  DiPIERRO, Michael, J. ,  THOMAS, Albert, V. ,  RILEY, David, A.

    IPC: C07H17/08

    CPC classification number: C07H17/08

    Abstract: A process for the preparation of 4''-deoxyerythromycins, having formula (I), wherein R is H or OH, Rp is H or acetyl, and R is H or loweralkyl; by treatment of the 2'-O-acetyl-4''-imidazolylthionocarbonyl-erythromycin starting material with the radical initiator 4,4'-azobis-(4-cyanovaleric acid), H3PO2 and an organic base in a water-miscible solvent other than an alcohol, and optionally eliminating the 2'-O-acetyl group. In a preferred embodiment, the water-miscible solvent is an alcohol and the deoxygenation and deacetylation is carried out in one step.

    Abstract translation: 制备具有式（I）的4“ - 脱氧红霉素的方法，其中R为H或OH，Rp为H或乙酰基，R 1为H或低级烷基; 通过用自由基引发剂4,4'-偶氮双（4-氰基戊酸），H 3 PO 2和有机碱在水混溶性溶剂中处理2'-O-乙酰基-4“ - 咪唑基硫羰基 - 红霉素原料 并且任选地除去2'-O-乙酰基。 在优选的实施方案中，水混溶性溶剂是醇，脱氧和脱乙酰化在一个步骤中进行。

    PREPARATION OF CRYSTAL FORM II OF CLARITHROMYCIN
    7.
    发明授权
    PREPARATION OF CRYSTAL FORM II OF CLARITHROMYCIN 无效
    生产的克拉霉素II晶体形态的

    公开(公告)号：EP0915899B1

    公开(公告)日：2004-08-04

    申请号：EP97934319.1

    申请日：1997-07-28

    Applicant: Abbott Laboratories

    Inventor： LIU, Jih-Hua ,  RILEY, David, A.

    IPC: C07H17/08

    CPC classification number: C07H17/08

    Abstract: The present invention provides a process for the preparation of 6-O-methylerythromycin A Form II comprising converting erythromycin A to 6-O-methylerythromycin A and treating the 6-O-methylerythromycin A with a number of common organic solvents or mixtures of common organic solvents.

    PROCESS FOR PREPARATION OF 4-DEOXYERYTHROMYCINS A AND B
    10.
    发明授权
    PROCESS FOR PREPARATION OF 4-DEOXYERYTHROMYCINS A AND B 失效
    制备4-脱氧红霉素A和B的方法

    公开(公告)号：EP1077987B1

    公开(公告)日：2004-04-28

    申请号：EP97950983.3

    申请日：1997-12-18

    Applicant: Abbott Laboratories

    Inventor： PAREKH, Shyamal, I. ,  GRAHAM, Alexandra, E. ,  DiPIERRO, Michael, J. ,  THOMAS, Albert, V. ,  RILEY, David, A.

    IPC: C07H17/08 ,  A61K31/70

    CPC classification number: C07H17/08

    Abstract: A process for the preparation of 4''-deoxyerythromycins, having formula (I), wherein R is H or OH, Rp is H or acetyl, and R is H or loweralkyl; by treatment of the 2'-O-acetyl-4''-imidazolylthionocarbonyl-erythromycin starting material with the radical initiator 4,4'-azobis-(4-cyanovaleric acid), H3PO2 and an organic base in a water-miscible solvent other than an alcohol, and optionally eliminating the 2'-O-acetyl group. In a preferred embodiment, the water-miscible solvent is an alcohol and the deoxygenation and deacetylation is carried out in one step.

    Abstract translation: 一种制备具有式（I）的4“ - 脱氧红霉素的方法，其中R是H或OH，Rp是H或乙酰基，并且R 1是H或低级烷基; 通过用自由基引发剂4,4'-偶氮双 - （4-氰基戊酸），H 3 PO 2和有机碱在水混溶性溶剂中处理2'-O-乙酰基-4“ - 咪唑基硫羰基 - 红霉素原料 比醇，并且任选地消除2'-O-乙酰基。 在一个优选的实施方案中，水混溶性溶剂是醇并且脱氧和脱乙酰一步进行。

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