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2005
Fused pyrimidine derivatives
Fused pyrimidine derivatives
R 0515
Efficient Synthesis of Bicyclic Oxazolino- and Thiazolino[3,2-c]pyrimidine-5,7-diand Its Application to the Synthesis of GnRH Antagonists. — The cycliza28- 168 ones
tion reaction of 2-alkyl substituted oxazolines (I) or thiazolines (IX) with chlorocarbonyl isocyanate (II) is used as key step in the rapid synthesis of human gonadotropin-releasing hormone (hGnRH) receptor antagonists for a SAR study. The reaction principle
is further broadened by its application to the synthesis of the novel bicyclic uracil derivative (XIV). — (PONTILLO*, J.; CHEN, C.; Bioorg. Med. Chem. Lett. 15 (2005)
5, 1407-1411; Dep. Med. Chem., Neurocrine Biosci., Inc., San Diego, CA 92121,
USA; Eng.) — H. Haber
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