519156-84-4

Upstream product

• 5000-65-7 2-bromo-3'-methoxyacetophenone 
• 308143-20-6 2-fluoromethyl-4-hydroxy-pyrimidine-5-carboxylic acid ethyl ester 

Downstream Products

• 519156-86-6 8-fluoro-1-(2-fluoro-benzyl)-7-(3-methoxy-phenyl)-4-oxo-1,4-dihydro-pyrrolo[1,2-a]pyrimidine-3-carboxylic acid ethyl ester 
• 519156-85-5 8-fluoro-7-(3-methoxy-phenyl)-4-oxo-1,4-dihydro-pyrrolo[1,2-a]pyrimidine-3-carboxylic acid ethyl ester 

Relevant academic research and scientific papers

A novel synthesis of 7-aryl-8-fluoro-pyrrolo[1,2-a]pyrimid-4-ones as potent, stable GnRH receptor antagonists.

A new class of small molecule GnRH antagonists, the 7-aryl-8-fluoro-pyrrolo[1,2-a]pyrimid-4-ones, was designed and a novel synthesis for these compounds was developed. The synthesis utilizes a base-catalyzed intramolecular cyclization of fluoromethyl pyrimidone 5 to generate the bicyclic core. Amongst the compounds synthesized, we discovered some highly potent GnRH receptor antagonists (e.g., 12, K(i)=9 nM), which showed enhanced stability towards acidic physiological conditions compared to the des-fluoro analogues.