352290-52-9

Upstream product

• 675605-94-4 5-bromo-1-(2,6-difluorobenzyl)-3-[2-(S)-N-Boc-aminopropyl]-6-methyluracil 
• 618914-13-9 1-(2,6-difluorobenzyl)-3-(3-oxobutyryl)urea 
• 352303-66-3 5-bromo-1-(2,6-difluoro-benzyl)-6-methyl-1H-pyrimidine-2,4-dione 
• 352303-65-2 N-1-(2,6-difluorobenzyl)-6-methyluracil 
• 17751-24-5 N-(2,6-difluorobenzyl) urea 
• 69385-30-4 2,6-difluorobenzylamine 
• 1044525-94-1 {2-[3-(2,6-difluoro-benzyl)-5-(2-fluoro-3-methoxy-phenyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-methyl-ethyl}-carbamic acid tert-butyl ester 

Relevant academic research and scientific papers

5-Aryluracils as potent GnRH antagonists-Characterization of atropisomers

Optimization of a series of uracils bearing a 2-fluoro- or 2-chloro-3-methoxyphenyl group at the 5-position resulted in compounds such as 3d and 3f with subnanomolar binding affinity at the human GnRH receptor. While the 2-fluoro-3-methoxyphenyl compound 3a was characterized as a mixture of interchangeable atropisomers, the diastereoisomers of 2-chloro-3-methoxyphenyl analogs were separated. It was found that the aR-atropisomer was much more potent than the aS-isomer based on the X-ray crystal structure of 3h-II.

Synthesis and Structure-Activity Relationships of 1-Arylmethyl-5-aryl-6-methyluracils as Potent Gonadotropin-Releasing Hormone Receptor Antagonists

Based on the SAR from bicyclic gonadotropin-releasing hormone (GnRH) antagonists such as 6-aminomethyl-7-aryl-pyrrolo [1,2-a] pyrimid-4-ones (5) and 2-aryl-3-aminomethyl-imidazolo-[1,2-a]pyrimid-5-ones (6a,b), a series of novel uracil compounds (8) were d