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    Intermediates for preparating non-peptide retroviral protease inhibitors
    6.
    发明公开
    Intermediates for preparating non-peptide retroviral protease inhibitors 失效
    用于制备非肽逆转录病毒蛋白酶抑制剂的中间体

    公开(公告)号：EP0839798A3

    公开(公告)日：1998-10-28

    申请号：EP97119700.9

    申请日：1990-05-17

    Applicant: ABBOTT LABORATORIES

    Inventor： Kempf, Dale J. ,  Norbeck, Daniel W. ,  Erickson, John W. ,  Sham, Hing Leung ,  Codacovi, Lynn M. ,  Plattner, Jacob J.

    IPC: C07C215/18 ,  C07C271/20 ,  C07C237/10 ,  C07D303/40 ,  C07D303/46

    Abstract: Intermediates, for preparing non-peptide retroviral protease inhibitors, said intermediates having the formula:
    or an acid addition salt thereof or an N-protected derivative thereof wherein at each occurrence the N-protecting group is independently selected from the group consisting of formyl, acetyl, pivaloyl, t-butylacetyl, t-butyloxycarbonyl, benzyloxycarbonyl, benzyl and isopropylaminocarbonyl; or said intermediates being selected from:
    (2S,3R,4S,5S)-2,5-di-(N-(Cbz-valinyl)amino)-3,4-dihydroxy-1,6-diphenylhexane; (2S,3S,4S,5S)-2,5-di-(N-(Cbz-valinyl)amino)-3,4-dihydroxy-1,6-diphenylhexane; (2S,3R,4R,5S)-2,5-di-(N-(Cbz-valinyl)amino)-3,4-dihydroxy-1,6-diphenylhexane; (2S,3S,4S,5S)-2,5-di-(N-(valinyl)amino)-3,4-dihydroxy-1,6-diphenylhexane; (2S,3R,4S,5S)-2,5-di-(N-(valinyl)amino)-3,4-dihydroxy-1,6-diphenylhexane; (2S,3R,4R,5S)-2,5-di-(N-(valinyl)amino)-3,4-dihydroxy-1,6-diphenylhexane; (2S,3S,4R,5S)-2-(N-(t-butyloxy)carbonyl)amino)-5-(N-(Cbz-valinyl)amino)-3,4-dihydroxy-1,6-diphenylhexane; 2-(N-benzyl-N-(benzyloxycarbonyl)amino)-5-(t-butyloxycarbonylamino)-1,6-diphenyl-3-hexene-3,4-oxide; 2-amino-5-(t-butyloxycarbonylamino)-1,6-diphenyl-3-hexene-3,4-oxide; and 2,5-di-(t-butyloxycarbonylamino)-1,6-diphenyl-3-hexene-3,4-oxide;
    or an acid addition salt thereof.

    Abstract translation: 用于制备非肽逆转录病毒蛋白酶抑制剂的中间体，所述中间体具有下式：或其酸加成盐或其N-保护的衍生物，其中在每次出现时N-保护基独立地选自甲酰基，乙酰基 ，新戊酰基，叔丁基乙酰基，叔丁氧基羰基，苄氧基羰基，苄基和异丙基氨基羰基; 或所述中间体选自：（2S，3R，4S，5S）-2,5-二 - （N-（Cbz-缬氨酰基）氨基）-3,4-二羟基-1,6-二苯基己烷; （2S，3S，4S，5S）-2,5-二 - （N-（Cbz基缬氨酰）氨基）-3,4-二羟基-1,6-二苯基己烷; （2S，3R，4R，5S）-2,5-二 - （N-（Cbz基缬氨酰）氨基）-3,4-二羟基-1,6-二苯基己烷; （2S，3S，4S，5S）-2,5-二 - （N-（缬氨酰基）氨基）-3,4-二羟基-1,6-二苯基己烷; （2S，3R，4S，5S）-2,5-二 - （N-（缬氨酰基）氨基）-3,4-二羟基-1,6-二苯基己烷; （2S，3R，4R，5S）-2,5-二 - （N-（缬氨酰基）氨基）-3,4-二羟基-1,6-二苯基己烷; （2S，3S，4R，5S）-2-（N-（叔丁氧基）羰基）氨基）-5-（N-（Cbz基缬氨酰）氨基）-3,4-二羟基-1,6-二苯基己烷; 2-（N-苄基-N-（苄氧羰基）氨基）-5-（叔丁氧羰）-1,6-二苯基 - 3-己烯-3,4-氧化物; 2-氨基-5-（叔丁氧羰）-1,6-二苯基 - 3-己烯-3,4-氧化物; 和2,5-二 - （叔丁氧基羰基氨基）-1,6-二苯基-3-己烯-3,4-氧化物; 或其酸加成盐。

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