8900
A. G. Cole et al. / Tetrahedron Letters 47 (2006) 8897–8900
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sponding purine derivative. The released quantities ran-
ged from 1.7 to 2.8 nmol per bead, corresponding to
yields of 54–89% (Table 1). In addition to good yields,
the purity level of the crude N-9-substituted dimino-
purines was exceptionally high.
8. (a) Dorff, P. H.; Garigipati, R. S. Tetrahedron Lett. 2001,
42, 2771–2773; (b) Norman, T. C.; Gray, N. S.; Koh, J. T.;
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This is exemplified by Figure 1, which shows the HPLC
profile at 220 nm of the purified analytical standard of
16a in comparison to the crude bead eluent (Fig. 1).16
In conclusion, a general and efficient solid-phase synthe-
sis of N-9-substituted 2,8-diaminopurines has been
developed. The synthesis performs well with a wide
range of R1, R2 and R3 components, and provides a
high level of both yield and purity. This route provides
an effective method for the construction of both parallel
and combinatorial N-9-substituted 2,8-diaminopurine
libraries.
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References and notes
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15. Microwave reactions were performed using a LAVIS-1000
multiQUANT irradiating at 500 W for 5 · 1 min with
15 min intervals between each irradiation.
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16. Analytical HPLC analysis was conducted using a PDA
linked Waters Millenium 2290 and Phenomenex Luna 3u
50 · 3 mm C8 column.
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