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Novel Procedure for the Coupling of Sterically Hindered Electron-Deficient Anilines to the 6-Position of the Purine Core |
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| Authors: | Ruben Leenders Jan Heeres Dirk Vandenput Jérôme Guillemont Paul Lewi |
| Institution: | 1. Mercachem BV , Nijmegen , the Netherlands ruben.leenders@mercachem.com;3. Janssen Research Foundation, Center for Molecular Design , Vosselaar , Belgium;4. Mercachem BV , Nijmegen , the Netherlands;5. Johnson and Johnson Pharmaceutical Research and Development, Medicinal Chemistry Department , Val de Reuil , France |
| Abstract: | Sterically hindered electron-deficient anilines are coupled to the 6-position of the purine core only when activated as their corresponding TFA-amide. The free anilines did not react under all conditions tested. After aqueous work-up, the TFA-group is lost. This procedure provides a new tool in the construction of purines functionalized with a sterically hindered electron-deficient aniline in the 6-position.  |
| Keywords: | Heterocycles HIV medicinal chemistry |