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Details for Patent: 5,659,045

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Details for Patent: 5,659,045

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), Zhao; Chen (Gurnee, IL), Sowin; Thomas J. (Grayslake, IL)
Assignee: Abbott Laboratories (Abbott Park, IL)
Filing Date:Apr 05, 1995
Application Number:08/417,295
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) C.sub.1 -to -C.sub.6 -loweralkyl, (iii) hydroxy, (iv) C.sub.1 -to-C.sub.6 -alkoxy and (v) C.sub.1 -to -C.sub.6 -thioalkoxy;

R.sub.6 is hydrogen or C.sub.1 -to -C.sub.6 -loweralkyl; and

R.sub.7 is thiazolyl, oxazolyl, isoxazolyl or isothiazolyl wherein the thiazolyl, oxazolyl, isoxazolyl or isothiazolyl ring is unsubstituted or substituted with C.sub.1 -to-C.sub.6 -loweralkyl; or an acid addition salt thereof, comprising (a) reacting a compound of the formula: ##STR19## wherein R.sub.4 and R.sub.4a are defined as above with (i) R*B(OH).sub.2 or ##STR20## wherein R* is phenyl, halo-substituted phenyl, dihalo-substituted phenyl, C.sub.1 -to-C.sub.6 -alkoxy-substituted phenyl, C.sub.1 -to -C.sub.6 -loweralkyl-substituted phenyl, bis-trifluormethyl-substituted phenyl or naphthyl or C.sub.1 -to-C.sub.6 -loweralkyl, followed by (b) acylating the product of step (a) 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.

2. The process of claim 1 wherein R.sub.4 and R.sub.4a are phenyl and R* is phenyl.

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 (a) reacting (2S,3S,5S)-2,5-diamino-1,6-diphenyl-3-hydroxyhexane with phenylboric acid, followed by (b) acylating the product of step (a) with ((5-thiazolyl)methyl)-(4-nitrophenyl)carbonate.

4. A process for the preparation of (2S,3S,5S)-5-Amino-1-phenyl-2-(N-((5-thiazolyl)methoxycarbonyl)amino)-6-(5 -thiazolyl)-3-hydroxyhexane or an acid addition salt thereof, comprising (a) reacting (2S,3S,5S)-2,5-Diamino-1-phenyl-6-(5-thiazolyl)-3-hydroxyhexane with phenylboric acid, followed by (b) acylating the product of step (a) with ((5-thiazolyl)methyl)-(4-nitrophenyl)carbonate.
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