Solid-Phase Synthesis of 2-Amino-7,8-dihydropteridin-6(5H)-ones

doi:10.1055/s-0029-1219285

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Synfacts 2010(3): 0361-0361
DOI: 10.1055/s-0029-1219285

Polymer-Supported Synthesis

Solid-Phase Synthesis of 2-Amino-7,8-dihydropteridin-6(5H)-ones

Contributor(s): Yasuhiro Uozumi, Yoichi M. A. Yamada
A. Metzger*, L.-Y. Qin, A. G. Cole, K. W. Saionz, M.-R. Brescia, H. Gstach, J. R. Wareing, J. Zimmermann, W. K.-D. Brill, J. J. Baldwin, R. E. Dolle, I. Henderson
Ligand Pharmaceuticals, Inc., Cranbury and Novartis Institutes for Biomedical Research, Cambridge, USA; Vienna, Austria and Basel, Switzerland

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Publikationsdatum:
18. Februar 2010 (online)

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Significance

A solid-phase synthesis of substituted 2-amino-7,8-dihydropteridin-6(5H)-ones 11 was described. Aminomethyl-terminated Argogel 1 was used as a solid support where the desired dihydropteridinones 11 were prepared via eleven SPOS steps (5 examples; 39-96% yield, 77-95% purity).