17880-61-4

Usage

Uses

Used in Organic Synthesis:
Methyl 5-ethynylpyridine-2-carboxylate is used as a building block in the preparation of various pharmaceuticals and agrochemicals. Its unique structure allows for the synthesis of a wide range of compounds with potential therapeutic and pesticidal properties.
Used in Chemical Research:
Methyl 5-ethynylpyridine-2-carboxylate is used as a reagent in chemical research. Its reactivity and functional groups make it a valuable tool for studying various chemical reactions and mechanisms.
Used in Material Science:
Methyl 5-ethynylpyridine-2-carboxylate has potential applications in the development of new materials and bioactive compounds. Its unique structure and properties can be utilized to create novel materials with specific characteristics and functions.
Used in Pharmaceutical Industry:
Methyl 5-ethynylpyridine-2-carboxylate is used as an intermediate in the synthesis of various pharmaceuticals. Its versatile structure allows for the development of new drugs with improved efficacy and selectivity.
Used in Agrochemical Industry:
Methyl 5-ethynylpyridine-2-carboxylate is used in the synthesis of agrochemicals, such as pesticides and herbicides. Its potential as a building block for these compounds can lead to the development of more effective and environmentally friendly products.
Safety Precautions:
Methyl 5-ethynylpyridine-2-carboxylate should be handled and stored according to proper safety protocols due to its potential health hazards and reactivity. Appropriate personal protective equipment and handling procedures should be followed to minimize risks associated with its use.

Upstream product

• 30766-11-1 5-bromoisonicotinic acid 
• 29682-15-3 methyl 5-bromopicolinate 

Downstream Products

• 1350553-45-5 methyl 5-((5-tert-butyl-2-(trifluoromethylsulfonyloxy)phenyl)ethynyl)picolinate 
• 1350553-48-8 methyl 5-((5-tert-butyl-2-((triisopropylsilyl)ethynyl)phenyl)ethynyl)picolinate 
• 1350553-51-3 methyl 5-((5-tert-butyl-2-ethynylphenyl)ethynyl)picolinate 
• 1350553-54-6 dimethyl 5,5'-(6,6'-(buta-1,3-diyne-1,4-diyl)bis(3-tert-butyl-6,1-phenylene)bis(ethyne-2,1-diyl))dipicolinate 
• 1350553-57-9 5,5'-(6,6'-(buta-1,3-diyne-1,4-diyl)bis(3-tert-butyl-6,1-phenylene)bis(ethyne-2,1-diyl))dipicolinic acid 

Relevant academic research and scientific papers

COMBINATION PRODUCT FOR THE TREATMENT OF CANCEROUS DISEASES

The present invention relates to a product for combination therapies useful for the treatment of cancer diseases. In particular, the invention relates to the combination of an anti-PD-Ll antibody and an MCT4 inhibitor of Formula (I). The therapeutic combination may be utilized for the use in treating a subject having a cancer disease that tests positive for PD-L1 and/or MCT4 expression.

DISUBSTITUTED ALKYNE DERIVATIVES

The present invention relates to disubstituted alkyne derivatives. These compounds are useful for the prevention and/or treatment of several medical conditions including hyperproliferative disorders and diseases.

Design, biological evaluation and X-ray crystallography of nanomolar multifunctional ligands targeting simultaneously acetylcholinesterase and glycogen synthase kinase-3

Both cholinesterases (AChE and BChE) and kinases, such as GSK-3α/β, are associated with the pathology of Alzheimer's disease. Two scaffolds, targeting AChE (tacrine) and GSK-3α/β (valmerin) simultaneously, were assembled, using copper(I)-catalysed azide alkyne cycloaddition (CuAAC), to generate a new series of multifunctional ligands. A series of eight multi-target directed ligands (MTDLs) was synthesized and evaluated in vitro and in cell cultures. Molecular docking studies, together with the crystal structures of three MTDL/TcAChE complexes, with three tacrine-valmerin hybrids allowed designing an appropriate linker containing a 1,2,3-triazole moiety whose incorporation preserved, and even increased, the original inhibitory potencies of the two selected pharmacophores toward the two targets. Most of the new derivatives exhibited nanomolar affinity for both targets, and the most potent compound of the series displayed inhibitory potencies of 9.5 nM for human acetylcholinesterase (hAChE) and 7 nM for GSK-3α/β. These novel dual MTDLs may serve as suitable leads for further development, since, in the micromolar range, they exhibited low cytotoxicity on a panel of representative human cell lines including the human neuroblastoma cell line SH-SY5Y. Moreover, these tacrine-valmerin hybrids displayed a good ability to penetrate the blood-brain barrier (BBB) without interacting with efflux pumps such as P-gp.

Design, synthesis and structure-activity relationship evaluation of novel LpxC inhibitors as Gram-negative antibacterial agents

LpxC inhibitors are new-type antibacterial agents developed in the last twenty years, mainly against Gram-negative bacteria infections. To develop novel LpxC inhibitors with good antibacterial activities and biological metabolism, we summarized the basic skeleton of reported LpxC inhibitors, designed and synthesized several series of compounds and tested their antibacterial activities against Escherichial coli and Pseudomonas aeruginosa in vitro. Structure-activity relationships have been discussed in this article. The metabolism stability of YDL-2, YDL-5, YDL-8, YDL-14, YDL-20–YDL-23 have been evaluated in liver microsomes, which indicated that the 2-amino isopropyl group may be a preferred structure than the 2-hydroxy ethyl group in the design of LpxC inhibitors.

ETHYNYLBENZENE DERIVATIVES

Disclosed are compounds of formulae (I), (II), and (II)I: and pharmaceutically acceptable salts thereof, wherein the variables, R, R1, R2, R3, R101, L, D, Q, Y, X, and Z are defined herein. These compounds are useful for treating Gram-negative bacteria infections.

Fluorogenic N,O-chelates built on a C2-symmetric aryleneethynylene platform: Spectroscopic and structural consequences of conformational preorganization and ligand denticity

Using π-extended aryleneethynylene as a rigid structural skeleton, a C2-symmetric bis(picolinate) ligand was prepared. Binding of zinc(II) or cadmium(II) ion to this formally tetradentate N2O 2-chelate resulted in significant red-shifts and enhancement in emission. The metal-ligand interaction responsible for such structural change was investigated by isolation and characterization of a tetrazinc(II) complex, in which the picolinate group functions not only as terminal bidentate but also as bridging with its μ-1,3 carboxylate unit.

Bi-aromatic compounds linked via a heteroethylene radical, and pharmaceutical and cosmetic compositions using them

Bi-aromatic compounds linked via a heteroethynylene radical are provided along with pharmaceutical and cosmetic compositions containing these compounds and methods for their use.

Bi-aromatic compounds linked via a heteroethylene radical, and pharmaceutical and cosmetic compositions using them

Bi-aromatic compounds linked via a heteroethynylene radical are provided along with pharmaceutical and cosmetic compositions containing these compounds and methods for their use.

Bi-aromatic compounds bound by a heteroethynylene radical and pharmaceutical and cosmetic compositions containing same

Bi-aromatic compounds linked via a heteroethynylene radical are provided along with pharmaceutical and cosmetic compositions containing these compounds and methods for their use.