36082-50-5Relevant articles and documents
The discovery of a potent and selective pyrazolo-[2,3-e]-[1,2,4]-triazine cannabinoid type 2 receptor agonist
Moir, Michael,Lane, Samuel,Montgomery, Andrew P.,Hibbs, David,Connor, Mark,Kassiou, Michael
, (2020/12/21)
The development of selective CB2 receptor agonists is a promising therapeutic approach for the treatment of inflammatory diseases, without CB1 receptor mediated psychoactive side effects. Preliminary structure-activity relationship studies on pyrazoylidene benzamide agonists revealed the -ylidene benzamide moiety was crucial for functional activity at the CB2 receptor. A small library of compounds with varying linkage moieties between the pyrazole and substituted phenyl group has culminated in the discovery of a potent and selective pyrazolo-[2,3-e]-[1,2,4]-triazine agonist 19 (CB2R EC50 = 19 nM, CB1R EC50 > 10 μM). Docking studies have revealed key structural features of the linkage group that are important for potent functional activity.
Preparation method of chloro-substituted polyhydroxy aza-aromatic ring compound (by machine translation)
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Paragraph 0019; 0020; 0021-0024, (2019/10/01)
The invention discloses a preparation method, namely BTC and SOCl, of a chloropolyhydroxyl aza heteroaromatic ring compound as a raw material with a polyhydroxy aza heteroaromatic ring compound as a raw material, and a preparation method thereof. 2 As the double chlorination reagent, a chloropolyhydroxyl aza-aromatic ring compound is produced by chlorination reaction with 4 - dimethylaminopyridine (DMAP) as a catalyst at room temperature to reflux temperature of the reaction, as a catalyst. BTC TC TC TC2 /DMDMAP chlorination system has high efficiency, high selectivity and chlorine substitution on a polyhydroxy nitrogen heterocyclic compound; the system can replace POCl3 , The production of phosphorus-containing wastewater is avoided. Using BTC as a chlorination reagent, the reaction by-product was HCl and CO. 2 . From the aspects of industrial wastewater treatment, environmental protection and the like, the advantages thereof are obvious; SOCl is distilled off after the reaction is ended. 2 The quantity is almost no loss, can be used repeatedly, and reduces the process cost. (by machine translation)
Preparation method for halogenated uracil compounds
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Paragraph 0039; 0041; 0043; 0044; 0045, (2018/08/04)
The invention discloses a preparation method for halogenated uracil compounds as shown in a formula 2 which is described in the specification. The preparation method comprises a step of subjecting a compound 1 and PCl5 to a chlorination reaction in a solvent. X in the formula is F, Cl, Br or I. The solvent is one or more selected from a group consisting of SOCl2, carbon tetrachloride, 1,2-dichloroethane, 1,1,1-trichloroethane, trichloroethylene and 1,1,2-trichloroethane. The preparation method uses 5-halouracil as a starting material, and is simple in process, high in yield, friendly to environment and suitable for industrial production.