152434-87-2

Upstream product

• 68-12-2 N,N-dimethyl-formamide 
• 152434-86-1 1-(benzyloxy)-2,4-difluorobenzene 
• 100-39-0 benzyl bromide 
• 367-27-1 2,4-difluorophenol 
• 100-44-7 benzyl chloride 

Relevant academic research and scientific papers

Substitution of terminal amide with 1H-1,2,3-triazole: Identification of unexpected class of potent antibacterial agents

3-Methoxybenzamide (3-MBA) derivatives have been identified as novel class of potent antibacterial agents targeting the bacterial cell division protein FtsZ. As one of isosteres for the amide group, 1,2,3-triazole can mimic the topological and electronic features of the amide, which has gained increasing attention in drug discovery. Based on these considerations, we prepared a series of 1H-1,2,3-triazole-containing 3-MBA analogues via isosteric replacement of the terminal amide with triazole, which had increased antibacterial activity. This study demonstrated the possibility of developing the 1H-1,2,3-triazole group as a terminal amide-mimetic element which was capable of both keeping and modulating amide-related bioactivity. Surprisingly, a different action mode of these new 1H-1,2,3-triazole-containing analogues was observed, which could open new opportunities for the development of antibacterial agents.

Macrocyclic compounds and methods for their production

There is provided inter alia compounds of formula (I): for use in treatment of viral infection or as an immunosuppressant.

Novel Dosage Form

There is provided inter alia a pharmaceutical dosage form for oral administration comprising a sanglifehrin as active ingredient in which the sanglifehrin active ingredient is protected from acid degradation in the stomach environment following oral admin

NOVEL DOSAGE FORM

There is provided inter alia apharmaceutical dosage form fororal administration comprising a sanglifehrin as active ingredient in which the sanglifehrin active ingredient is protected from acid degradation in the stomach environment following oral adminis

PYRROLO[2,3-B] PYRIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS

Compounds of formula III which are active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.

Syntheses of 2,5- and 2,6-Difluoronorepinephrine, 2,5-Difluoroepinephrine, and 2,6-Difluorophenylephrine: Effect of Disubstitution with Fluorine on Adrenergic Activity

Synthetic routes to difluorinated analogs of the adrenergic agonists, norepinephrine (NE), epinephrine (E), and phenylephrine (PE) have been developed.The syntheses were based on elaboration of the ethanolamine side chains from the appropriately polyfunctionalized benzaldehydes.The benzaldehydes were prepared from precursor difluorinated benzenes by sequential regioselective lithiations and reaction with electrophiles to introduce hydroxyl and carboxaldehyde functionalities.Binding and functional assay data demonstrate that the 2,6-difluorinated analogs are relatively inactive at both α- and β-adrenergic receptors.These results are consistent with earlier observations that 2-fluoro substitution of adrenergic agonists decreases α-adrenergic activity whereas 6-fluoro substitution decreases β-adrenergic activity.