- Bromine-Lithium Exchange on Bromo-8-hydroxyquinolines via Formation of their Sodium Salts.
-
A short and versatile method is reported for the preparation of 8-hydroxyquinoline derivatives by reaction of n-butyllithium with 5,7-dibromo-8-hydroxyquinoline 2 and 7-bromo-8-hydroxyquinoline 1 as their sodium salts.Thus, bromine-lithium exchange reaction on compound 2, highly regioselective, gave after addition of various electrophiles, 5-substituted 7-bromo-8-hydroxyquinolines 4a-j in moderate to good yields.The same procedure was also applicable to 7-bromo-8-hydroxyquinoline 1 which led to 7-substituted 8-hydroxyquinolines 3a-b.
- Mongin, Florence,Fourquez, Jean-Marie,Rault, Stephanie,Levacher, Vincent,Godard, Alain,et al.
-
-
Read Online
- Aza-and polyaza-naphthalenly ketones useful as hiv integrase inhibitors
-
Certain aza- and polyaza-naphthalenyl ketones including certain quinolinyl and naphthyridinyl ketones are described as inhibitors of HIV integrase and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HIV and the treatment or the delay in the onset of AIDS, as compounds or pharmaceutically acceptable salts, or as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.
- -
-
Page/Page column 43
(2010/02/10)
-
- NITROGEN-CONTAINING HETEROARYL COMPOUNDS HAVING HIV INTEGRASE INHIBITORY ACTIVITY
-
A compound of the formula (I): wherein Z4, Z5 and Z9 each is independently carbon atom or nitrogen atom; Y is hydroxy, mercapto or amino; RA is a group of the formula: (wherein C ring is nitrogen-containing heteroaryl) has an inhibitory activity against integrase.
- -
-
-
