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|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|
|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 (i) C.sub.1 -to-C.sub.6 -loweralkyl, (ii) C.sub.2 -to-C.sub.6 -loweralkenyl, (iii) C.sub.3 -to-C.sub.7 -cycloalkyl, (iv) C.sub.3 -to-C.sub.7 -cycloalkyl-C.sub.1 -to-C.sub.6 -alkyl, (v) C.sub.5 -to-C.sub.7 -cycloalkenyl and (vi) C.sub.5 -to-C.sub.7 -cycloalkenyl-C.sub.1 -to-C.sub.6 -alkyl; |
n is 1, 2 or 3;
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;
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; and
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;
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) reacting the product of step (a) with a compound of the formula: ##STR21## or an activated ester derivative thereof, wherein R.sub.1, R.sub.2, R.sub.3, Z and n 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. The process of claim 1 wherein R.sub.1 is monosubstituted thiazolyl, monosubstituted oxazolyl, monosubstituted isoxazolyl or monosubstituted isothiazolyl wherein the substituent is C.sub.1 -to-C.sub.6 -loweralkyl, n is 1, Z is --O--, --S-- or --N(R.sub.8)-- wherein R.sub.8 is C.sub.1 -to-C.sub.6 -loweralkyl, R.sub.2 is hydrogen, R.sub.4 and R.sub.4a are phenyl and R* is phenyl.
4. The process of claim 1 wherein R.sub.1 is monosubstituted thiazolyl or monosubstituted oxazolyl wherein the substituent is C.sub.1 -to-C.sub.6 -loweralkyl, n is 1, Z is --N(R.sub.8)-- wherein R.sub.8 is C.sub.1 -to-C.sub.6 -loweralkyl, R.sub.2 is hydrogen, R.sub.4 and R.sub.4a are phenyl and R* is phenyl.
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