457628-40-9

Usage

Uses

Used in Organic Chemistry:
2-amino-5-trimethylsilanylethynylpyridine serves as a building block in the synthesis of a variety of organic molecules, particularly those with applications in the biological and pharmaceutical sectors. Its presence of the trimethylsilane group enhances its reactivity, allowing it to participate in multiple chemical reactions to yield a broad spectrum of functionalized derivatives.
Used in Medicinal Chemistry and Drug Discovery:
In the realm of medicinal chemistry, 2-amino-5-trimethylsilanylethynylpyridine is utilized for its unique chemical properties, which make it a valuable tool in the research and development of new drugs. Its potential in drug discovery is attributed to the compound's ability to be modified and functionalized, offering a wide range of possibilities for the creation of novel therapeutic agents.

Upstream product

• 1072-97-5 5-bromo-2-pyridylamine 
• 1066-54-2 trimethylsilylacetylene 
• 20511-12-0 2-amino-5-iodopyridine 
• 936342-51-7 2-nitro-5-trimethylsilanylethynyl-pyridine 

Downstream Products

• 1428445-69-5 C₂₅H₂₇F₃N₈O 
• 911115-16-7 5-[2-[7-(trifluoromethyl)-5-[4-(trifluoromethyl)phenyl]pyrazolo[1,5-a]pyrimidin-3-y1]ethynyl]-2-pyridinamine 

Relevant academic research and scientific papers

Ru(II)-polypyridine complexes with alkynyl Schiff base ligand: influence of π-conjugation, donor/acceptor substituents, and counter anions on electrochemical, luminescence, and catalytic properties

Ru(II)-polypyridine complexes of the general formula [Ru(L1/L2)(phen)2]X2 (1a–6a) and [Ru(L1/L2)(bipy)2]X2 (1b–6b) (where X = ClO4, BF4, PF6; phen = 1,10-phenanthroline, bipy = 2,2′-bipyridine) were prepared by the reaction of [Ru(phen)2Cl2]·2H2O and [Ru(bipy)2Cl2]·2H2O with (E)-5-((4-methoxyphenyl)ethynyl)-N-(pyridin-2-ylmethylene)pyridin-2-amine (L1) and (E)-5-((4-nitrophenyl)ethynyl)-N-(pyridin-2-ylmethylene)pyridine-2-amine (L2) in the presence of NaBF4, NaClO4, and NaPF6. The electrochemical properties of all the complexes indicate reversible redox behavior corresponding to Ru(II)–Ru(III) couple and are susceptible to variation of electron-donating/accepting properties of substituent group on L1 and L2. All complexes showed room temperature luminescence corresponding to π→π* intra-ligand charge-transfer (ILCT) transition with chelation enhanced fluorescence and is finely tuned by increasing π-conjugation, size of counter anions, and variation of substituent group with different electronic effects in the complexes. All the complexes worked as an effective catalyst for the oxidation of benzyl alcohol to corresponding benzaldehyde in good yield at room temperature. (Figure presented.).

Ruthenium(II)-2, 2′-bipyridine/1, 10-phenanthroline complexes incorporating (E)-2-(((5-((4-methoxyphenyl)ethynyl)pyridin-2-yl)imino)methyl)-4-((4-nitro phenyl)ethynyl)phenol as a ligand

A new series of hexa-coordinated Ru(II) complexes of the type [Ru(L)(phen)2]X (1a–d) and [Ru(L)(bipy)2]X (2a–d) (where phen = 1,10-phenanthroline, bipy = 2,2′-bipyridine, X = NO3, BF4, ClO4, PF6) have been prepared by the reaction of (E)-2-(((5-((4-methoxyphenyl)ethynyl)pyridin-2-yl)imino)methyl)-4-((4-nitrophenyl)ethynyl)phenol (L) with [Ru(phen)2]Cl2·2H2O and [Ru(bipy)2]Cl2·2H2O. The complexes were characterized by physico-chemical and spectroscopic methods. All complexes are 1:1 conducting and diamagnetic in nature. In acetonitrile solution, the complexes displayed one reversible Ru(II)–Ru(III) oxidation couple and one irreversible Ru(III)–Ru(IV) oxidation and are sensitive to π-acidic character of phen and bipy ligands. The complexes show room-temperature luminescence originated from the lowest energy metal-to-ligand charge transfer excited state and are sensitive to difference in size of the counter anions. All the complexes displayed second harmonic generation by Kurtz-powder technique indicating their potential for the application as a useful NLO material.

COMPOUNDS AND METHODS FOR TREATING CANCER

Substituted cinnamamide compounds and analogs, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat, prevent or ameliorate cancer are provided.

ALKYNYL INDAZOLE DERIVATIVE AND USE THEREOF

The main object of the present invention is to provide a novel compound which has a VEGF receptor tyrosine kinase inhibitory activity and is useful as an active ingredient for the treatment of diseases accompanying angiogenesis or edema, for example, age-related macular degeneration or the like. The present invention includes, for example, an alkynyl indazole derivative represented by the following general formula (I), a pharmaceutical acceptable salt thereof, and a medicine containing thereof.

Pyrimidine or pyridine pyridine ketone compound and its preparation method and application (by machine translation)

The invention discloses a kind of type I of the pyrimidine or pyridine pyridine ketone compound and its preparation and application, which belongs to the technical field of pharmaceutical preparation. The compounds have high-efficient and selectively inhibit the cell cycle dependent kinases (Cdks) CDK4 and CDK6 active, and then by inhibiting CDK4/CDK6 prevent tumor cell division. Therefore, the compounds of this invention can be used for CDK4 and CDK6 the involved in cell cycle control disorders result in various diseases, especially suitable for the treatment of malignant tumors. (by machine translation)

METHODS FOR THE PREPARATION OF 5-[2-[7 (TRIFLUOROMETHYL)-5-[4- (TRIFLUOROMETHYL)PHENYL]PYRAZOLO [1,5-A]PYRIMIDIN-3-YL]ETHYNYL]-2-PYRIDINAMINE

The present invention provides methods for preparing 5-[2-[7-(trifluoromethyl)-5-[4-(trifluoromethyl)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]ethynyl]-2-pyridinamine (compound A), which is useful for the treatment of depression and other CNS disorders. The present methods are useful for preparing compound A on large scale in manufacturing facilities.

Rapid discovery of a novel series of Abl kinase inhibitors by application of an integrated microfluidic synthesis and screening platform

Drug discovery faces economic and scientific imperatives to deliver lead molecules rapidly and efficiently. Using traditional paradigms the molecular design, synthesis, and screening loops enforce a significant time delay leading to inefficient use of data in the iterative molecular design process. Here, we report the application of a flow technology platform integrating the key elements of structure-activity relationship (SAR) generation to the discovery of novel Abl kinase inhibitors. The platform utilizes flow chemistry for rapid in-line synthesis, automated purification, and analysis coupled with bioassay. The combination of activity prediction using Random-Forest regression with chemical space sampling algorithms allows the construction of an activity model that refines itself after every iteration of synthesis and biological result. Within just 21 compounds, the automated process identified a novel template and hinge binding motif with pIC50 > 8 against Abl kinase - both wild type and clinically relevant mutants. Integrated microfluidic synthesis and screening coupled with machine learning design have the potential to greatly reduce the time and cost of drug discovery within the hit-to-lead and lead optimization phases.

5-ALKYNYL-PYRIMIDINES

The present invention encompasses compounds of general formula (1) wherein R1 to R4 R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.

5-ALKYNYL-PYRIMIDINES

The present invention encompasses compounds of general formula (1) wherein R1 to R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.

NEW TRIAZOLYLPHENYL SULFONAMIDES AS SERINE/THREONINE KINASE INHIBITORS

The present invention encompasses compounds of general formula (I) wherein the groups R2 to R4, A,X and m are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, pharmaceutical preparations which contain compounds of this kind and their use as medicaments.