28690-95-1

Upstream product

• 100-02-7 4-nitro-phenol 
• 3140-73-6 2-chloro-4,6-dimethoxy-1 ,3,5-triazine 
• 1124-31-8 potassium 4-nitrophenolate 

Downstream Products

• 21002-15-3 2-phenyloxy-4,6-dimethoxy-1,3,5-triazine 
• 100-02-7 4-nitro-phenol 
• 42030-76-2 4-((4,6-dimethoxy-1,3,5-triazin-2-yl)oxy)benzaldehyde 
• 33950-59-3 2-(4-methylphenoxy)-4,6-dimethoxy-1,3,5-triazine 
• 42030-75-1 1-(4-((4,6-dimethoxy-1,3,5-triazin-2-yl)oxy)phenyl)ethanone 
• 67-56-1 methanol 
• 1075-59-8 2-hydroxy-4,6-dimethoxy-1,3,5-triazine 
• 241483-00-1 4-(4,6-dimethoxy-1,3,5-triazin-2-yl)-4-morpholine 

Relevant academic research and scientific papers

FUSED-CYCLIC PYRAZOLONE FORMAMIDE COMPOUND AND PREPARATION METHOD THEREFOR, PHARMACEUTICAL COMPOSITION AND USE THEREOF

Provided are a class of fused-cyclic pyrazolone formamide compounds and a preparation method therefor, a pharmaceutical composition and the use thereof. Specifically, provided is a compound having the structure as shown in formula (I) (with each group defined in the description). The compound can be used as an AXL inhibitor in the preparation of a pharmaceutical composition for treating tumors.

Nickel-catalyzed Suzuki-Miyaura coupling of heteroaryl ethers with arylboronic acids

Nickel-catalyzed Suzuki-Miyaura coupling of heteroaryl ethers with arylboronic acids was described. Selective activation of the phenol C-O bonds was achieved by converting them into the corresponding aryl 2,4-dimethoxy-1,3,5- triazine-6-yl ethers, in which aryl C-O bond could be selectively cleaved with inexpensive, air-stable NiCl2(dppf) as a catalyst. Coupling of these readily accessible heteroaryl ethers proved tolerant of extensive functional groups.

NOVEL INDOL CARBOXYLIC ACID BISPYRIDYL CARBOXAMIDE DERIVATIVES, PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, PREPARATION METHOD AND COMPOSITION CONTAINING THE SAME AS AN ACTIVE INGREDIENT

Disclosed herein are a new indole carboxylic acid bispyridyl carboxamide derivative, a preparation method thereof, and a composition for prevention or treatment of obesity, urinary disorders, and CNS disorders, containing the same as an active ingredient. Because the indole carboxylic acid bispyridyl carboxamide derivatives according to the present invention have high affinity for 5-HT2c receptors, act selectively on the 5-HT2c receptors, the derivatives rarely have adverse effects caused by other receptors. Because the derivatives effectively inhibit serotonin activity, they may be useful for treatment or prevention of obesity; urinary disorders such as urinary incontinence, premature ejaculation, erectile dysfunction, and prostatic hyperplasia; CNS disorders such as depression, anxiety, concern, panic disorder, epilepsy, obsessive-compulsive disorder, migraine, sleep disorder, withdrawal from drug abuse, Alzheimer's disease, and schizophrenia, associated with 5-HT2c receptors.

Novel indol carboxylic acid bispyridyl carboxamide derivatives as 5-HT2c receptor antagonists

Disclosed herein are a new indole carboxylic acid bispyridyl carboxamide derivative, a preparation method thereof, and a composition for prevention or treatment of obesity, urinary disorders, and CNS disorders, containing the same as an active ingredient. Because the indole carboxylic acid bispyridyl carboxamide derivatives according to the present invention have high affinity for 5-HT2c receptors, act selectively on the 5-HT2c receptors, the derivatives rarely have adverse effects caused by other receptors. Because the derivatives effectively inhibit serotonin activity, they may be useful for treatment or prevention of obesity; urinary disorders such as urinary incontinence, premature ejaculation, erectile dysfunction, and prostatic hyperplasia; CNS disorders such as depression, anxiety, concern, panic disorder, epilepsy, obsessive-compulsive disorder, migraine, sleep disorder, withdrawal from drug abuse, Alzheimer's disease, and schizophrenia, associated with 5-HT2c receptors.

NOVEL INDOL CARBOXYLIC ACID BISPYRIDYL CARBOXAMIDE DERIVATIVES, PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, PREPARATION METHOD AND COMPOSITION CONTAINING THE SAME AS AN ACTIVE INGREDIENT

Disclosed herein are a new indole carboxylic acid bispyridyl carboxamide derivative, a preparation method thereof, and a composition for prevention or treatment of obesity, urinary disorders, and CNS disorders, containing the same as an active ingredient. Because the indole carboxylic acid bispyridyl carboxamide derivatives according to the present invention have high affinity for 5-HT2c receptors, act selectively on the 5-HT2c receptors, the derivatives rarely have adverse effects caused by other receptors. Because the derivatives effectively inhibit serotonin activity, they may be useful for treatment or prevention of obesity; urinary disorders such as urinary incontinence, premature ejaculation, erectile dysfunction, and prostatic hyperplasia; CNS disorders such as depression, anxiety, concern, panic disorder, epilepsy, obsessive-compulsive disorder, migraine, sleep disorder, withdrawal from drug abuse, Alzheimer's disease, and schizophrenia, associated with 5-HT2c receptors.

Stepwise versus concerted mechanisms at trigonal carbon: Transfer of the 1,3,5-triazinyl group between aryl oxide ions in aqueous solution

Displacements of 4-nitrophenolate ions from 2-(4-nitrophenoxy)-4,6-dimethoxy-1,3,5-triazine by substituted phenolate ions in aqueous solution obey a linear Br?nsted-type equation, log kArO = 0.951pKa - 10.98, over a range of pKa values greater than and less than the pKa of the leaving phenol. The absence of curvature is consistent with a mechanism involving a single transition state. This conclusion is supported by the existence of cross-correlation effects (Pxy = 0.0561) on βnuc of the pKa of the leaving group and on β1g of the pKa of the nucleophile on β1g. The value of βeq, the Br?nsted selectivity for transfer of the triazinyl function between phenolate ions, is calculated from the Br?nsted data to be 1.48. The identity reaction of 3,4-dinitrophenolate ion with the (3,4-dinitrophenoxy)triazine is calculated to have a Kreevoy-Albery τ value of 1.04, indicating that in this case changes in effective charge on entering and leaving ligands are approximately balanced.

Prediction of Acylation Capability of s-Triazinyl (Active) Esters Based on Structures of Appropriate Ethers. Crystal Structures of Two 2-Aryloxy-4,6-dimethoxy-1,3,5-triazines: 2-(2-Ethoxycarbonylphenoxy)-4,6-dimethoxy-1,3,5-triazine and 2-(4-Methylphenoxy)-4,6-dimethoxy-1,3,5-triazine

C(O)-OR bond length (R=aromatic system) determines activity of an ester in acylation reaction.Attempts were made to correlate its value with O-R bond lengths of appropriate ether.Crystal structures of two 2-aryloxy-4,6-dimethoxy-1,3,5-triazines have been determined.Key words: Active esters, X-ray structures, structure-reactivity relationship, aryloxy-s-triazins, s-triazinyl esters