申请人:ABBOTT LABORATORIES
公开号:EP0839798A2
公开(公告)日:1998-05-06
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.
用于制备非肽类逆转录病毒蛋白酶抑制剂的中间体,所述中间体具有以下式子:
或其酸加成盐或其 N-保护衍生物,其中每次出现时,N-保护基独立选自甲酰、乙酰、特戊酰、叔丁基乙酰、叔丁氧羰基、苄氧羰基、苄基和异丙氨基羰基组成的组;或所述中间体选自以下物质
(2S,3R,4S,5S)-2,5-二(N-(Cbz-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-苄氧羰基缬氨酰氨基)-3,4-二羟基-1,6-二苯基己烷;
(2S,3R,4R,5S)-2,5-二(N-苄氧羰基缬氨酰氨基)-3,4-二羟基-1,6-二苯基己烷;
(2S,3S,4S,5S)-2,5-二(N-(缬氨酰)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)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)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-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-(叔丁氧羰基氨基)-1,6-二苯基-3-己烯-3,4-氧化物;
2-氨基-5-(叔丁氧羰基氨基)-1,6-二苯基-3-己烯-3,4-氧化物;以及
2,5-二(叔丁氧羰基氨基)-1,6-二苯基-3-己烯-3,4-氧化物;
或其酸加成盐。