Traceless solid-phase synthesis of N1,N7-disubstituted purines |
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| Authors: | Fu Han Lam Yulin |
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| Institution: | Department of Chemistry, National University of Singapore, 3 Science Drive 3, Singapore 117543. |
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| Abstract: | A highly regioselective and traceless solid-phase route to N1,N7-disubstituted purines has been developed. Key steps in the reaction strategy involves (i) coupling of 6-chloropurine to the REM resin (Michael addition), (ii) oxidation, (iii) N1-alkylation, (iv) quaternization, and (v) product release through Hofmann elimination. A library of 15 N1,N7-disubstituted purines was synthesized. |
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