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2005
Uracil derivatives
R 0520
Synthesis and Structure—Activity Relationships of Uracil Derived Human GnRH
Antagonists: (R)-3-[2-(2-Amino)phenethyl]-1-(2,6-difluoroben02- 158 Receptor
zyl)-6-methyluracils Containing a Substituted Thiophene or Thiazole at C-5. —
The synthesis of the title antagonists such as (VIII) and (XIII) is achieved via a novel
and convenient preparation of uracil derivative (V). Urea (III) reacts with diketene (IV)
in the presence of trimethylsilyl chloride to give (V) in one step as the only product,
without a separate, acid-catalyzed cyclodehydration of the expected N-acetoacetylurea.
A thienyl or a thiazolyl group at C-5 is required for optimal receptor binding. Inclusion
of a 5-chloro substituent at the 2-thienyl group provides compound (VIIIc) with the
highest single digit nanomolar binding affinity for the human GnRH receptor. —
(ROWBOTTOM*, M. W.; et al.; Bioorg. Med. Chem. Lett. 14 (2004) 19, 4967-4973;
Dep. Med. Chem., Neurocrine Biosci., Inc., San Diego, CA 92121, USA; Eng.) —
H. Hoennerscheid
2005
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