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2005
Triazine derivatives
R 0655
A Convenient One-Pot Synthesis of Asymmetric 1,3,5-Triazine-2,4,6-triones
Its Application Towards a Novel Class of Gonadotropin-Releasing Hormone
25- 160 and
Receptor Antagonists. — A novel method for the preparation of asymmetric 1,3-dialkyl-1,3,5-triazine-2,4,6-triones (IV) from alkyl- or aryl-isocyanates (I), primary
amines (II) and N-chlorocarbonyl isocyanate (III) is reported. Subsequent alkylation
with N-protected amino alcohols, e.g. (V), using Mitsunobu conditions affords the target compounds, e.g. (VI), in good yields. — (GUO*, Z.; WU, D.; ZHU, Y.-F.; TUCCI,
F. C.; PONTILLO, J.; SAUNDERS, J.; XIE, Q.; STRUTHERS, R. S.; CHEN, C.;
Bioorg. Med. Chem. Lett. 15 (2005) 3, 693-698; Dep. Med. Chem., Neurocrine
Biosci., Inc., San Diego, CA 92121, USA; Eng.) — M. Paetzel
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