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Chemical Libraries for Analogs of Tamiflu and Relenza by D.O.S. Let our mother diamine be ‘transformed’ to analogs of tamiflu (oseltamivir) and relenza (zanamivir) in one or two steps.
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Copyright © 2009 DiaminoPharm Inc. All right reserved |
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mother diamine crystal |
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Tamiflu from Roche and Relenza from GSK are two of the most widely used drugs against swineflu (H1N1) and birdflu (H5N1). They have also been shown to be effective for treating seasonal flu. These two drugs are structurally related and can be classified as g,d-(S,S)-diamino acids. In general this class of compounds is difficult to synthesize in enantiomerically pure form. Tamiflu and Relenza themselves require many steps to synthesize and would be problematic for mass production in case of a pandemic.1 It would also be a challenge to synthesize tamiflu analogs to fight off resistance.
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A short and convergent approach to making tamiflu and relenza would be of great interest over the long and linear one.1 We recently showed how the mother diamine can be transformed to daughter diamines in a highly convergent manner by using the diaza-Cope rearrangement (DCR) process.2 More recently, we developed a one pot reaction for making a wide variety of g,d-(S,S)-diamino acids in enantiomerically pure form. For more information, please contact info@diaminopharm.com References 1. Magano, J. (2009) Chem. Rev. 109, 4398-4438. 2. (a) Kim, H.; So, S. M.; Kim, B. M.; Chin, J. (2008) Aldrichimica Acta, 77-88. (b) , H.; Nguyen,Y.; Yen,C. P.-H.; Chagal, L.; Lough, A. J.; Kim, B. M.; Chin, J. (2008) J. Am. Chem. Soc. 130, 12184-12191. |
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