10402-57-0

Upstream product

• 63157-19-7 (1-benzofuran-2-yl)(4-methoxyphenyl)methanone 
• 2491-38-5 2-bromo-1-(4'-hydroxyphenyl)-1-ethanone 
• 90-02-8 salicylaldehyde 
• 2632-13-5 2-Bromo-4'-methoxyacetophenone 
• 89-95-2 2-methyl-benzyl alcohol 
• 108-95-2 phenol 

Downstream Products

• 1262243-49-1 C₁₅H₁₂O₃ 

Relevant academic research and scientific papers

An expedient synthesis of enantioenriched substituted (2-benzofuryl) arylcarbinols via tandem Rap-Stoermer and asymmetric transfer hydrogenation reactions

An expedient synthesis of enantioenriched substituted (benzofuran-yl)-aryl and heteroaryl carbinols, is described. A key feature of this protocol is synthesis of functionally varied benzofuran scaffolds via a Rap-Stoermer reaction/catalytic asymmetric tra

Benzophenone derivatives and related compounds as potent histamine H3-receptor antagonists and potential PET/SPECT ligands

Para-substituted aromatic ethers with benzophenone or related structural elements and a 3-(1H-imidazol-4-yl)propyloxy moiety were prepared by Mitsunobu-type ether synthesis or SNAr reaction. Most of the title compounds possess high antagonist potency in histamine H3-receptor assays in vitro as well as in vivo in mouse CNS following oral administration. After defining 4-(3-(1H-imidazol-4-yl)propyloxy)phenyl phenyl methanone as a new lead, structure-activity relationships were investigated for this new class of compounds. Substitution of the meta′-position of the benzophenone moiety with halogen atoms (e.g., iodine, fluorine) led to compounds with high antagonist potency in vitro as well as in vivo (Ki = 9.3 and 4.3 nM, ED50 = 0.7 and 0.47 mg/kg p.o., 18 and 12, respectively). A receptor profile of several functional in vitro assays for several biogenic amine receptors for the meta′-iodinated derivative demonstrated high selectivity toward the histamine H3 receptor.