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Generated: August 19, 2017

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Title: HIV protease inhibitors useful for the treatment of AIDS
Abstract:Compounds of formula ##STR1## where A is usually carbonyl or --CH.sub.2 --, D is usually --CH.sub.2 --; R.sup.1 and R.sup.2 are independently hydrogen or optionally-substituted C.sub.1-4 alkyl or aryl, or R.sup.1 and R.sup.2 are joined together to form a monocyclic or bicyclic ring system, are HIV protease inhibitors. These compounds are useful in the prevention or treatment of infection by HIV and in the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
Inventor(s): Vacca; Joseph P. (Telford, PA), Dorsey; Bruce D. (Harleysville, PA), Guare; James P. (Quakertown, PA), Holloway; M. Katharine (Lansdale, PA), Hungate; Randall W. (Lansdale, PA), Levin; Rhonda B. (Lafayette Hill, PA), Huff; Joel R. (Gwynedd Valley, PA)
Assignee: Merck & Co., Inc. (Rahway, NJ)
Filing Date:Dec 04, 1996
Application Number:08/759,203
Claims:1. A process for making a compound of the formula I ##STR273## comprising reacting a compound (i) of the formula ##STR274## with R.sup.1 --X; wherein R.sup.1 is C.sub.1-4 alkyl unsubstituted or substituted with one or more of

(1) aryl unsubstituted or substituted with one or more of C.sub.1-4 alkyl, amino, hydroxy or aryl;

(2) a 5-7 membered cycloalkyl group unsubstituted or substituted with one or more of halo, C1-3 alkoxy or aryl; or

(3) heterocycle unsubstituted or substituted with one or more of oxo, halo, C.sub.1-4 alkoxy, C.sub.1-4 alkyl, --C(O)OC.sub.1-3 alkyl, --NHC(O)C.sub.1-3 alkyl, or Boc; and

X is selected from Cl, Br or I;

to give the compound of formula I.

2. The process of claim 1, wherein

R.sup.1 is C.sub.1-4 alkyl unsubstituted or substituted with a heterocycle wherein the heterocycle is unsubstituted or substituted with one or more of oxo, halo, C.sub.1-4 alkoxy, C.sub.1-4 alkyl, --C(O)OC.sub.1-3 alkyl, --NHC(O)C.sub.1-3 alkyl, or Boc.

3. The process of claim 2, wherein

R.sup.1 is C.sub.1-4 alkyl substituted with a heterocycle, wherein the heterocycle is selected from piperidinyl, pyridyl, thienyl, pyrrolyl, thiazolyl, imidazolyl, furyl, benzimidazolyl, pyrazinyl, isoxazolyl, pyridazinyl, or quinolinyl, and wherein the heterocycle is unsubstituted or substituted with one or more of oxo, halo, C.sub.1-4 alkoxy, C.sub.1-4 alkyl, --C(O)OC.sub.1-3 alkyl, --NHC(O)C.sub.1-3 alkyl, or Boc.

4. The process of claim 3 for making a compound J of the formula ##STR275## comprising reacting a compound (i) of the formula ##STR276## with a compound of the formula ##STR277## to give the compound J.

5. The process of claim 4 for making a compound J of the formula ##STR278## comprising reacting a compound (i) of the formula ##STR279## with 3-picolyl chloride to give the compound J.

6. A compound (i) of the formula: ##STR280## or a salt thereof.
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