186449-56-9

Upstream product

• 97025-00-8 2-hydroxy-4-oxo-2-phenethyl-valeric acid 
• 186449-48-9 5-hydroxy-5-methyl-3-(2-phenylethyl)-2(5H)-furanone 
• 500370-17-2 2-hydroxy-4-oxo-2-phenethylpentanoic acid ethyl ester 

Downstream Products

• 500370-14-9 3-chloro-6-methyl-4-phenethylpyridazine 

Relevant academic research and scientific papers

ANTIVIRAL AGENT

The present invention provides an integrase inhibitor. The inventors have have found the following compound of formula (I) possessing an integrase inhibitory activity. (wherein, R C and R D taken together with the neighboring carbon atoms form a ring which may be a condensed ring, Y is hydroxy, mercapto or amino; Z is O, S or NH ; R A is a group shown by (wherein, C ring is N-containing aromatic heterocycle) or the like)

Dehydration of 2-(2-arylethyl)-2-hydroxy-4-oxopentanoic acids and their hydrazones to form heterocycles

Dehydration of 2-(2-arylethyl)-2-hydroxy-4-oxopentanoic acids 1 with hydrochloric acid/acetic acid, affords 3-(2-arylethyl)-5-hydroxy-5-methyl-2(5H)-furanones4. Compounds of type 1 and 4 represent suitable precursors for the formation of pyridazin-3-ones 7 as they smoothly react with hydrazine. A new series of s-triazolo[4,3-b]pyridazin-3-ones 12 and tetrazolo[1,5-b]pyridazines 15 are obtained from the 3-chloropyridazines 11 upon treatment with semicarbazide and sodium azide, respectively. Reaction of 11 with phenyl- acetyl-hydrazine provides 3-benzyl-6-phenyl-8-(2-phenyl- ethyl)-s-triazolo[4,3-b]pyridazine 13 via dehydrative cyclization of the intermediate 14 which was clarified to exhibit tautomeric equilibria between enol-hydrazine form A and keto-hydrazine form B by means of 1H and 13C NMR spectroscopy. Attempts to synthesize 3-alloxy-pyridazines 18 by reacting 11 with sodium alloxide afford N-allyl compounds 17. Johann Ambrosius Barth 1997.