107128-47-2

Upstream product

• 403-32-7 (4-fluorophenyl)glyoxal 
• 2582-30-1 aminoguanidine bicarbonate 
• 79-17-4 aminoguanidine 
• 403-42-9 1-(4-fluorophenyl)ethanone 
• 447-43-8 1-(4-fluorophenyl)-2,2-dihydroxyethan-1-one 

Downstream Products

• 1321514-06-0 6-(2-chloro-6-methylpyridin-4-yl)-5-(4-fluorophenyl)-1,2,4-triazin-3-amine 
• 1321514-52-6 6-(2,6-dimethylpyridin-4-yl)-5-(4-fluorophenyl)-1,2,4-triazin-3-amine 
• 1321517-59-2 6-bromo-5-(4-fluorophenyl)-1,2,4-triazin-3-amine 
• 1321515-56-3 5-(4-fluorophenyl)-6-[2-methyl-6-(trifluoromethyl)pyridin-4-yl]-1,2,4-triazin-3-amine 

Relevant academic research and scientific papers

Multikilogram-Scale Preparation of AZD4635 via C-H Borylation and Bromination: The Corrosion of Tantalum by a Bromine/Methanol Mixture

An efficient route to AZD4635 has been developed utilizing the Suzuki-Miyaura reaction of a boronate ester prepared by C-H borylation on a multikilogram scale. Preparation of the cross-coupling partner using bromine/pyridine/methanol has highlighted the incompatibility of this reagent/solvent combination with tantalum, which is commonly used in the construction and repair of standard manufacturing vessels.

SUBSTITUTED ARYL COMPOUND AND PREPARATION METHOD THEREFOR AND USE THEREOF

The present application relates to a substituted aryl compound or a pharmaceutically acceptable salt, a stereoisomer, a polymorph, a solvate, a N-oxide, an isotope-labeled compound, a metabolite or a prodrug thereof, and a preparation method therefor and use thereof, also relates to a pharmaceutical composition containing the compound and a therapeutic use thereof. The compound or a pharmaceutical composition thereof can inhibit the activity of adenosine A2a receptor, and can be used for treating or preventing a disease related to adenosine A2a receptor, especially for treating a tumor.

1,2,4-TRIAZINE-4-AMINE DERIVATIVES

According to the invention there is provided a compound of formula A1 which may be useful in the treatment of a condition or disorder ameliorated by the inhibition of the A1- A2b or, particularly, the A2a receptor wherein the compound of formula A1 has the structure, wherein, A represents Cy1 or HetA; Cy1 represents a 5- to 14-membered aromatic, fully saturated or partially unsaturated carbocyclic ring system comprising one, two or three rings, which Cy1 group is optionally substituted by one or more R4a substituents; HetA represents a 5- to 14-membered heterocyclic group that may be aromatic, fully saturated or partially unsaturated, and which contains one or more heteroatoms selected from O, S and N, which heterocyclic group may comprise one, two or three rings and which HetA group is optionally substituted by one or more R4b substituents; B represents a Cy2 or HetB; Cy2 represents a 3- to 10-membered aromatic, fully saturated or partially unsaturated carbocyclic ring system comprising one or two rings, which Cy2 group is optionally substituted by one or more R4c substituents; HetB represents a 3- to 10-membered heterocyclic group that may be aromatic, fully saturated or partially unsaturated, and which contains one or more heteroatoms selected from O, S and N, which heterocyclic group may comprise one or two rings and which HetB group is optionally substituted by one or more R4d substituents.

FACILE SYNTHESIS OF FLUORINE CONTAINING IMIDAZO TRIAZINES THROUGH α-OXO-N-ARYL-α ARYLETHANEHYDRAZONOYL BROMIDES

Treatment of fluorine containing arylglyoxals with aminoguanidine bicarbonate in aqueous ethanol formed fluorinated 3-amino-5-aryltriazines which in turn on treatment with α-oxo-N-aryl-α-arylethanehydrazonoyl bromides afforded 3,6-diaryl-7-arylazoimidazo triazines in 75-80percent yield.All the compounds were characterized by their analytical and spectral (IR, PMR and Mass) data.Mass fragmentation patterns of these compounds have also been discussed.The screening of biological activities are in progress.