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    Key intermediates in the manufacture of simvastatin
    26.
    发明授权
    Key intermediates in the manufacture of simvastatin 失效
    辛伐他汀制造中的关键中间体

    公开(公告)号：US5763653A

    公开(公告)日：1998-06-09

    申请号：US816574

    申请日：1997-03-13

    Applicant: Jag Mohan Khanna ,  Yatendra Kumar ,  Rajesh Kumar Thaper ,  Satyananda Misra ,  S. M. Dileep Kumar

    Inventor： Jag Mohan Khanna ,  Yatendra Kumar ,  Rajesh Kumar Thaper ,  Satyananda Misra ,  S. M. Dileep Kumar

    IPC: C07C231/00 ,  C07C235/30 ,  C07D309/30 ,  C07C67/02

    CPC classification number: C07C235/30 ,  C07D309/30 ,  C07C2101/02 ,  C07C2102/28

    Abstract: A process for preparing simvastatin from lovastatin or mevinolinic acid in salt form comprises treating either starting material with cyclopropyl or butyl amine, the pyranone ring thereby being opened when lovastatin is the starting material, adding a methyl group to the 2-methylbutyrate side chain, and thereafter closing the open pyranone ring to produce simvastatin. The process is performed without protecting and deprotecting the two hydroxy groups of the open pyranone ring. In a preferred embodiment, the starting material is treated with cyclopropyl amine which produces simvastatin via the novel intermediate lovastatin cyclopropyl amide.

    Abstract translation: 以盐形式从洛伐他汀或甲维林酸制备辛伐他汀的方法包括用环丙基或丁胺处理起始原料，当洛伐他汀为原料时，吡喃酮环由此开放，向2-甲基丁酸酯侧链加入甲基， 然后关闭开放的吡喃酮环以产生辛伐他汀。 在不保护和去保护开放式吡喃酮环的两个羟基的情况下进行该方法。 在优选的实施方案中，用环丙胺处理起始物质，其通过新的中间体洛伐他汀环丙基酰胺产生辛伐他汀。

    PROCESS FOR THE PREPARATION OF ATAZANAVIR OR ITS BISULFATE SALT
    27.
    发明申请
    PROCESS FOR THE PREPARATION OF ATAZANAVIR OR ITS BISULFATE SALT 审中-公开
    制备ATAZANAVIR或其BISULFATE盐的方法

    公开(公告)号：US20140343290A1

    公开(公告)日：2014-11-20

    申请号：US14235127

    申请日：2012-07-25

    Applicant: Rakesh Kumar Singh ,  Nagaraju Gottumukkala ,  Mahavir Singh Khanna ,  Rajesh Kumar Thaper ,  Mohan Prasad ,  Sudershan Kumar Arora

    Inventor： Rakesh Kumar Singh ,  Nagaraju Gottumukkala ,  Mahavir Singh Khanna ,  Rajesh Kumar Thaper ,  Mohan Prasad ,  Sudershan Kumar Arora

    IPC: C07D213/42

    CPC classification number: C07D213/42

    Abstract: The present invention relates to an improved process for the preparation of atazanavir bisulfate, an inhibitor of retroviral aspartate protease. The process of the present invention comprises conversion of 1,1-dimethylethyl[(2S,3R)-4-chloro-3-hydroxy-phenylbutan-2-yl]carbamate (Formula II) into 1-[4-(pyridine-2-yl)-phenyl]-4(S)-5 hydroxy-2-N-tert-butoxycarbonylamino-5(S)—N—(N-methoxycarbonyl-(L)-tert-leucyl)amino-6-phenyl-2-azahexane (Formula VII) without isolating intermediate compounds formed therein, followed by its subsequent conversion to atazanavir or its bisulfate salt.

    Abstract translation: 本发明涉及一种制备逆转录病毒天冬氨酸蛋白酶抑制剂阿扎那韦硫酸氢盐的改进方法。 本发明的方法包括将[（2S，3R）-4-氯-3-羟基 - 苯基丁-2-基]氨基甲酸酯（式II）的1,1-二甲基乙基酯转化为1- [4-（吡啶-2 - 基） - 苯基] -4（S）-5-羟基-2-N-叔丁氧基羰基氨基-5（S）-N-（N-甲氧基羰基 - （L） - 叔 - 亮氨酰基）氨基-6-苯基-2 （式Ⅶ），而不分离其中形成的中间体化合物，随后转化成阿扎那韦或其硫酸氢盐。

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