Traceless solid-phase synthesis of N1,N7-disubstituted purines.
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.
Fu
Han
H
Department of Chemistry, National University of Singapore, 3 Science Drive 3, Singapore 117543.
Lam
Yulin
Y
D020650:Combinatorial Chemistry Techniques / Q000379:methods*; D011687:Purines / Q000138:chemical synthesis* / Q000737:chemistry*
D011687:Purines