Publisher： Bentham Science Publishers
E-ISSN： 1875-6255|6|2|130-133
ISSN： 1570-1786
Source： Letters in Organic Chemistry, Vol.6, Iss.2, 2009-03, pp. : 130-133
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Abstract
An analogue of Tipranavir was designed by replacing the dihydropyrone core with a 1,3-cyclohexanedione ring. The thio-alkyl group was used as a temporary protection group for , &bgr;-unsaturated cyclohexane-1,3-diketone derivative, and the resulting compound was reacted with an ethyl-organometallic reagent to form the desired Michael addition product. By using this strategy, a more stable analogue of Tipranavir was synthesized and exhibited excellent HIV protease inhibition (12 nM Ki).
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