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Details for Patent: 5,616,720

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Details for Patent: 5,616,720

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), Reno; Daniel S. (Kenosha, WI)
Assignee: Abbott Laboratories (Abbott Park, IL)
Filing Date:Apr 06, 1995
Application Number:08/418,056
Claims:1. A process for the preparation of a compound of the formula: ##STR18## wherein R.sub.1 is monosubstituted thiazolyl, monosubstituted oxazolyl, monosubstituted isoxazolyl or monosubstituted isothiazolyl wherein the substituent is selected from C.sub.1 -to-C.sub.6 -loweralkyl;

n is 1, 2 or 3;

R.sub.2 is hydrogen or C.sub.1 -to-C.sub.6 -loweralkyl;

R.sub.3 is C.sub.1 -to-C.sub.6 -loweralkyl;

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.5 -loweralkyl,

(iii) hydroxy,

(iv) C.sub.1 -to-C.sub.6 -alkoxy or benzyloxy and

(v) C.sub.1 -to-C.sub.6 -thioalkoxy or benzyl-S-;

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

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; and

Z is absent, --O--, --S--, --CH.sub.2 -- or --N(R.sub.8)-- wherein R.sub.8 is C.sub.1 -to-C.sub.6 -loweralkyl, C.sub.3 -to-C.sub.7 -cycloalkyl, --OH or --NHR.sub.8a wherein R.sub.8a is hydrogen or C.sub.1 -to-C.sub.6 -loweralkyl; or a pharmaceutically acceptable salt thereof, comprising (a) reacting a compound of the formula: ##STR19## wherein R.sub.4 and R.sub.4a are as defined above with Ti(OR****).sub.4 wherein R**** is C.sub.1 -to-C.sub.6 -loweralkyl, followed by reaction with a compound of the formula: ##STR20## or an activated ester derivative thereof, wherein R.sub.1, R.sub.2, R.sub.3, Z and n are as defined above to give a compound of the formula: ##STR21## and (b) acylation of 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.1 is C.sub.1 -to-C.sub.6 -loweralkyl-substituted thiazolyl, R.sub.2 is hydrogen, R.sub.3 is C.sub.1 -to-C.sub.6 -loweralkyl, R.sub.4a and R.sub.4 are phenyl, R.sub.6 is hydrogen, R.sub.7 is thiazolyl and n is 1.

3. The process of claim 1 wherein R**** is isopropyl.

4. The process of claim 1 wherein R.sub.1 is 2-isopropyl-4-thiazolyl, n is 1, R.sub.2 is hydrogen, R.sub.3 is isopropyl, R.sub.4 and R.sub.4a are phenyl, R.sub.6 is hydrogen, R.sub.7 is 5-thiazolyl, Z is --N(CH.sub.3)-- and R**** is isopropyl.
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