HIV protease inhibitors are among the most powerful drugs in suppressing HIV in human patients. However, HIV developed resistance to all protease inhibitor drugs so far marketed or used in clinical trials. HIV generates resistance by mutating its protease. The strains of HIV containing mutant proteases less vulnerable to inhibitor drug are able to replicate better and maintain the infection. No effective principle exists for the design of resistance-proof HIV protease inhibitors (HIVPr). A new inhibitor has been developed based on a new concept for designing resistance invulnerable HIVPr inhibitors. In vitro data have shown that this inhibitor is effective against many known HIVPr mutants resistant to other HIVPr inhibitor drugs. The new concept is, therefore, generally applicable for the design of other resistance invulnerable HIVPr inhibitor drugs.
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Page/Page column 8
(2010/02/14)
A practical regiospecific synthesis of ortho- and meta-hydroxybenzenesulfonic acids
The first regiospecific route to the ortho-hydroxybenzenesulfonic acid and competitive way to its meta regioisomer are reported.Both compounds were obtained from the silylation of the corresponding chlorophenols, followed by sulfonation of the arylsilane intermediates.Keywords: silylation / sulfonation / chlorophenols / hydroxybenezensulfonic acids
Babin, P.,Bennetau, B.,Bourgeois, P.,Rajarison, F.,Dunogues, J.
p. 25 - 28
(2007/10/02)
Process for aryl-quinone and aryl-naphthoquinone diazide sulfonic acids
A process for the preparation of aryl-diazide-sulfonic acids by a series of sequential in-situ process steps. The process comprises the nitrosation of a hydroxyarylsulfonic acid; conversion of the nitroso-derivative to a sulfamate which is then diazotized to the diazide. Temperature and pH are maintained in predetermined ranges to maintain the reaction products in solution without the formation side-products or the need to isolate intermediates. The process of the invention is particularly useful in the preparation of light-sensitive materials such as naphthoquinonediazide sulfonic acids which are used in the preparation of photoresist compositions. The invention provides a high purity product at a high material efficiency, high equipment utilization, low effluent discharge, and reduced cost.