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    Process for preparing piperazinepentaneamide HIV protease inhibitors
    1.
    发明授权
    Process for preparing piperazinepentaneamide HIV protease inhibitors 失效

    公开(公告)号：US06649761B2

    公开(公告)日：2003-11-18

    申请号：US10158527

    申请日：2002-05-30

    申请人： Norihiro Ikemoto ,  Jinchu Liu

    发明人： Norihiro Ikemoto ,  Jinchu Liu

    IPC分类号： C07D41306

    CPC分类号： C07D413/14

    摘要： A process for preparing &ggr;-hydroxy-4-[[2-oxazolyl]alkyl]-&agr;-[(cyclo)alkyl- or aryl- or heteroaryl-substituted methyl]-2-[[(un)substituted alkyl]aminocarbonyl]-1-piperazinepentanamides is disclosed. The piperazinepentanamides are useful as HIV protease inhibitors. A process for making a 4-[[2-oxazolyl]alkyl]-2-[[(un)substituted alkyl]aminocarbonyl]piperazine by treating a ketoamide precursor with fuming sulfuric acid in the presence of polyphosphoric acid is also disclosed. In addition, a process for enhancing the optical purity of 4-[[2-oxazolyl]alkyl]-2-[[(un)substituted alkyl]aminocarbonyl]-piperazines via the formation 2-naphthalenesulfonic acid crystal salts thereof is disclosed, as well as a method for purifying 2-naphthalenesulfonic acid.

    Enzymatic process of making alpha 1a adrenergic receptor antagonists using protease
    2.
    发明授权
    Enzymatic process of making alpha 1a adrenergic receptor antagonists using protease 失效
    使用蛋白酶制备α1a肾上腺素能受体拮抗剂的酶学方法

    公开(公告)号：US06207444B1

    公开(公告)日：2001-03-27

    申请号：US09122301

    申请日：1998-07-24

    申请人： Daniel R. Sidler ,  Michel Chartrain ,  Norihiro Ikemoto ,  Gerald F. Bills ,  Christopher Roberge ,  Colleen S. Taylor

    发明人： Daniel R. Sidler ,  Michel Chartrain ,  Norihiro Ikemoto ,  Gerald F. Bills ,  Christopher Roberge ,  Colleen S. Taylor

    IPC分类号： C12P1712

    CPC分类号： C07D239/22 ,  C07D401/04 ,  C07D401/14

    摘要： This invention relates to crystalline pharmaceutically acceptable salts of an alpha 1a adrenergic receptor antagonist, Compound A, which are useful in the treatment of benign prostatic hyperplasia. Pharmaceutical compositions employing the crystalline salts, and processes for making and using the crystalline salts and pharmaceutical compositions of Compound A are also disclosed. This invention further relates to a process for obtaining enantiomerically pure intermediate useful for the synthesis of end product alpha 1a adrenergic receptor antagonists. The end product compounds are useful for the treatment of benign prostatic hyperplasia and for relaxing lower urinary tract tissue. The invention also relates to a process for preparing a class of dihydropyrimidinone compounds of which Compound A is a member, wherein the process involves deprotonating a dihydropyrimidinone compound and then coupling the deprotonated derivative with a primary amine.

    摘要翻译： 本发明涉及可用于治疗良性前列腺增生的α1α肾上腺素能受体拮抗剂，化合物A的结晶药学上可接受的盐。 还公开了使用结晶盐的药物组合物，以及制备和使用化合物A的结晶盐和药物组合物的方法。 本发明还涉及用于获得可用于合成终产物α1α肾上腺素能受体拮抗剂的对映体纯中间体的方法。 最终产品化合物可用于治疗良性前列腺增生和放松下尿路组织。 本发明还涉及一种制备其中化合物A为成员的一类二氢嘧啶酮化合物的方法，其中该方法包括使二氢嘧啶酮化合物去质子化，然后将去质子化衍生物与伯胺偶联。

    Process for the preparation cis-(1S,2R)-indanediol by direduction of 1,2-indanedione using trichosporon cutaneum
    4.
    发明授权
    Process for the preparation cis-(1S,2R)-indanediol by direduction of 1,2-indanedione using trichosporon cutaneum 失效
    通过使用trichosporon cutaneum引导1,2-茚满酮制备顺式 - （1S，2R） - 茚满二醇的方法

    公开(公告)号：US06171832B2

    公开(公告)日：2001-01-09

    申请号：US09300344

    申请日：1999-04-27

    申请人： Michael M. Chartrain ,  Norihiro Ikemoto ,  Anthony O. King

    发明人： Michael M. Chartrain ,  Norihiro Ikemoto ,  Anthony O. King

    IPC分类号： C12P722

    CPC分类号： C12P7/18 ,  Y10S435/911

    摘要： A process for preparing cis-(1S,2R)-indanediol is disclosed. The process comprises (A) fermenting a culture medium containing a yeast strain selected from the group consisting of Trichosporon cutaneum MY 1506 (ATCC 74440) and mutants thereof and 1,2-indanedione to form cis-(1S,2R)-indanediol; and (B) recovering cis-(1S,2R)-indanediol from the culture medium. A process for preparing (1S)-amino-(2R)-indanol from the recovered cis-(1S,2R)-indanediol via the Ritter reaction is also disclosed.

    摘要翻译： 公开了制备顺式 - （1S，2R） - 1,2-二醇的方法。 该方法包括（A）发酵含有选自Trichosporon cutaneum MY 1506（ATCC 74440）及其突变体和1,2-茚二酮的酵母菌株以形成顺式 - （1S，2R） - 茚满二醇的培养基; 和（B）从培养基中回收顺式 - （1S，2R） - 1,2-二醇。 还公开了通过Ritter反应从回收的顺式 - （1S，2R） - 1,2-二醇制备（1S） - 氨基 - （2R） - 茚满的方法。