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2005
Fused pyrimidine derivatives
R 0515
Quinazolinethiones and Quinazolinediones, Novel Inhibitors of Inosine MonoDehydrogenase: Synthesis and Initial Structure—Activity Relation25- 151 phosphate
ships. — Amino ester (I) are converted to isothiocyanates (III), followed by reaction
with amines (IV) to give the title compounds (V) after cyclization. The approach to
obtain analogous quinazolinediones suffers from the instability of the corresponding
isocyanates and so an alternative sequence based on solid-phase techniques is developed (no yields given). — (HAUGHAN*, A. F.; et al.; Bioorg. Med. Chem. Lett. 15
(2005) 3, 751-754; Celltech R&D Ltd., Granta Park, Cambridge CB1 6GS, UK;
Eng.) —M. Paetzel
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