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Details for Patent: 6,667,404

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Details for Patent: 6,667,404

Title: Retroviral protease inhibiting compounds
Abstract:A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed.
Inventor(s): Kempf; Dale J. (Libertyville, IL), Norbeck; Daniel W. (Crystal Lake, IL), Sham; Hing Leung (Gurnee, IL), Zhao; Chen (Gurnee, IL), Sowin; Thomas J. (Grayslake, IL), Reno; Daniel S. (Kenosha, WI), Haight; Anthony R. (Park City, IL)
Assignee: Abbott Laboratories (Abbott Park, IL)
Filing Date:Feb 07, 2003
Application Number:10/360,325
Claims:1. A process for the preparation of a compound of the formula: ##STR18##

or an N-protected derivative thereof; wherein R.sub.4 and R.sub.4a are independently selected from phenyl, thiazolyl and oxazolyl wherein the phenyl, thiazolyl and oxazolyl ring is unsubstituted or substituted with a substituent selected from the group consisting of (i) halo, (ii) loweralkyl, (iii) hydroxy, (iv) alkoxy and (v) thioalkoxy; R.sub.6 is hydrogen or loweralkyl; and R.sub.7 is thiazolyl, oxazolyl, isoxazolyl or isothiazolyl wherein the thiazolyl, oxazolyl, isoxazolyl or isothiazolyl ring is unsubstituted or substituted with loweralkyl, comprising reacting a compound of the formula: ##STR19##

or an N-protected derivative thereof wherein R.sub.4a and R.sub.4 are as defined above with an acylating compound of the formula: ##STR20## wherein R.sub.6 and R.sub.7 are as defined above; and L is an activating group for an acylation reaction.

2. The process of claim 1 wherein R.sub.4a and R.sub.4 are phenyl, R.sub.6 is hydrogen and R.sub.7 is thiazolyl, oxazolyl, isoxazolyl or isothiazolyl.

3. The process of claim 1 wherein R.sub.4a and R.sub.4 are phenyl, R.sub.6 is hydrogen and R.sub.7 is thiazolyl.

4. The process of claim 1 wherein wherein L is p-nitrophenyl, phenyl, N-succinimidyl, N-phthalimidyl, N-benzotriazolyl, N-5-norbornene-2,3-carboxamidyl or 2,4,5-trichlorophenyl.

5. A process for the preparation of (2S,3S,5S)-5-amino-2-(N-((5-thiazolyl)methoxycarbonyl)amino)-1,6-diphenyl- 3-hydroxyhexane or an N-protected derivative thereof, comprising reacting (2S,3S,5S)-- 2,5-diamino-1,6-diphenyl-3-hydroxyhexane or an N-protected derivative thereof with an acylating compound of the formula: ##STR21##

wherein L is an activating group for the acylation reaction.

6. The process of claim 5 wherein L is p-nitrophenyl, phenyl, N-succinimidyl, N-phthalimidyl, N-benzotriazolyl, N-5-norbornene-2,3-carboxamidyl or 2,4,5-trichlorophenyl.

7. The process of claim 5 wherein L is p-nitrophenyl.

8. The process of claim 5 wherein L is phenyl.

9. The process of claim 5 wherein L is N-succinimidyl.

10. The process of claim 5 wherein L is N-phthalimidyl.

11. The process of claim 5 wherein L is N-benzotriazolyl.

12. The process of claim 5 wherein L is N-5-norbornene-2,3-carboxamidyl.

13. The process of claim 5 wherein L is 2,4,5-trichlorophenyl.

14. A process for the preparation of (2S,3S,5S)-5-(t-butyloxycarbonylamino)-2-(N-((5-thiazolyl)methoxycarbonyl) amino)-1,6-diphenyl-3-hydroxyhexane, comprising reacting (2S,3S,5S)-- 2-amino-5-(t-butyloxycarbonylamino)-1,6-diphenyl-3-hydroxyhexane with an acylating compound of the formula: ##STR22##

wherein L is an activating group for the acylation reaction.

15. The process of claim 14 wherein L is p-nitrophenyl, phenyl, N-succinimidyl, N-phthalimidyl, N-benzotriazolyl, N-5-norbornene-2,3-carboxamidyl or 2,4,5-trichlorophenyl.

16. The process of claim 14 wherein L is p-nitrophenyl.

17. The process of claim 14 wherein L is phenyl.

18. The process of claim 14 wherein L is N-succinimidyl.

19. The process of claim 14 wherein L is N-phthalimidyl.

20. The process of claim 14 wherein L is N-benzotriazolyl.

21. The process of claim 14 wherein L is N-5-norbornene-2,3-carboxamidyl.

22. The process of claim 14 wherein L is 2,4,5-trichlorophenyl.

23. (2S,3S,5S)-5-(t-butyloxycarbonylamino)-2-(N-((5-thiazolyl)methoxycarbonyl) amino)-1,6-diphenyl-3-hydroxyhexane.
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