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Details for Patent: 5,565,418

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Details for Patent: 5,565,418

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 L. (Gurnee, IL), Zhao; Chen (Gurnee, IL), Sowin; Thomas J. (Grayslake, IL), Reno; Daniel S. (Kenosha, IL), Allen; Michael S. (Silver Lake, WI), Copper; Arthur J. (Lake Villa, IL), Tien; Jien-Heh J. (Libertyville, IL)
Assignee: Abbott Laboratories (Abbott Park, IL)
Filing Date:Apr 05, 1995
Application Number:08/417,304
Claims:1. A process for the preparation of a compound of the formula: ##STR18## wherein R.sub.4 and R.sub.4a are independently selected from phenyl, thiazolyl and oxazolyl wherein the phenyl, thiazolyl or oxazolyl ring is unsubstituted or substituted with a substituent selected from

(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; or an acid addition salt thereof, comprising reacting a compound of the formula: ##STR19## wherein R.sub.4 and R.sub.4a are defined as above with a compound of the formula (R.sub.6)(R.sub.7)CHOC(O)OL wherein L is an activating group for the acylation reaction and wherein R.sub.6 and R.sub.7 are defined as above, followed by N-deprotection.

2. The process of claim 1 wherein R.sub.4 and R.sub.4a are phenyl and L is p-nitrophenyl.

3. A process for the preparation of (2S,3S,5S)-5-Amino-2-(N-((5-thiazolyl)methoxycarbonyl)amino)-1,6-diphenyl- 3-hydroxyhexane or an acid addition salt thereof, comprising reacting (2S,3S,5S)-5-(t-Butyloxycarbonylamino)-2(N-((5-thiazolyl)methoxycarbonyl)a mino)-1,6-diphenyl-3-hydroxyhexane with 5-(p-nitrophenyloxycarbonyloxymethyl)thiazole, followed by N-deprotection.
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