97289-74-2

Upstream product

• 1694-31-1 tert-butyl acetoacetate 
• 62-53-3 aniline 

Downstream Products

• 959996-08-8 tert-butyl 3-(phenylamino)butanoate 
• 1449480-47-0 tert-butyl 5-(2-methoxyphenyl)-2-methyl-1-phenyl-1H-pyrrole-3-carboxylate 
• 1572039-08-7 tert-butyl 5-methyl-1,2-diphenyl-1H-imidazole-4-carboxylate 
• 1572039-07-6 C₂₁H₂₁ClN₂O₂ 

Relevant academic research and scientific papers

5-Hydroxyindole-based EZH2 inhibitors assembled via TCCA-catalyzed condensation and Nenitzescu reactions

5-Hydroxyindole derivatives have various demonstrated biological activities. Herein, we used 5-hydroxyindole as a synthetic starting point for structural alterations in a combinatorial process to synthesize 22 different compounds with EZH2 inhibitor pharmacophores. A series of 5-hydroxyindole-derived compounds were screened inhibitory activities against K562 cells. According to molecular modeling and in vitro biological activity assays, the preliminary structure-activity relationship was summarized. Compound L–04 improved both the H3K27Me3 reduction and antiproliferation parameters (IC50 = 52.6 μM). These findings revealed that compound L–04 is worthy of consideration as a lead compound to design more potent EZH2 inhibitors. During the preparation of compounds, we discovered that trichloroisocyanuric acid (TCCA) is a novel catalyst which demonstrates condensation-promoting effects. To gain insight into the reaction, in situ React IR technology was used to confirm the reactivity. Different amines were condensed in high yields with β-diketones or β-ketoesters in the presence of TCCA to afford the corresponding products in a short time (10~20 min), which displayed some advantages and provided an alternative condensation strategy.

TBAI or KI-Promoted Oxidative Coupling of Enamines and N-Tosylhydrazine: An Unconventional Method toward 1,5- and 1,4,5-Substituted 1,2,3-Triazoles

A novel method for the synthesis of 1,5- and 1,4,5-substituted 1,2,3-triazoles has been reported. This approach is promoted by iodine-TBHP oxidation system using enamines and N-tosylhydrazine as materials, which avoid the dependence of traditional methods on azides and transition metals. Through this approach, various 1,5- and 1,4,5-substituted 1,2,3-triazoles were delivered in moderate to high yields. The mechanistic study indicated that an amino exchange would be involved in the reaction process. Moreover, the product methyl 1-(2-methoxyphenyl)-4-methyl-1H-1,2,3-triazole-5-carboxylate is a useful precursor to anti-influenza A agent, and further application research was conducted. (Figure presented.).

Oxidative cross-coupling/cyclization to build polysubstituted pyrroles from terminal alkynes and β-enamino esters

A novel silver-mediated highly selective synthesis of polysubstituted pyrroles by the C-H/C-H oxidative cross-coupling/cyclization of terminal alkynes with β-enamino esters has been developed. This protocol represents a simple, efficient and selective way to construct polysubstituted pyrroles in good yields from basic chemical materials.

Pyridone derivatives as NK3 antagonists

The present invention relates to compounds useful in therapy, in particular in the treatment of psychosis, to compositions comprising said compounds, and to methods of treating diseases comprising the administration of said compounds.

PYRIDONE DERIVATIVES AS NK3 ANTAGONISTS

The present invention relates to compound of formula (I) useful in therapy, in particular in the treatment of psychosis, to compositions comprising said compounds, and to methods of treating diseases comprising the administration of said compounds.