90101-20-5

Usage

Uses

Used in Pharmaceutical Industry:
(4-METHYL-PYRIDIN-2-YL)-CARBAMIC ACID TERT-BUTYL ESTER is used as an immunomodulatory and disease-modifying agent for the treatment of multiple sclerosis. It is utilized to reduce inflammation and damage to the central nervous system by inhibiting the production of inflammatory cytokines and immune cells.
Used in Neurological Treatments:
(4-METHYL-PYRIDIN-2-YL)-CARBAMIC ACID TERT-BUTYL ESTER is used as a therapeutic agent for neurological conditions, specifically targeting multiple sclerosis. It helps in managing the disease by reducing the activity of the immune system that leads to inflammation and damage in the central nervous system.
Used in Patient Monitoring:
(4-METHYL-PYRIDIN-2-YL)-CARBAMIC ACID TERT-BUTYL ESTER is used as a reference for monitoring patients taking the medication for potential liver toxicity and to ensure proper dosing through regular blood tests, which helps in evaluating any adverse effects and maintaining patient safety.

InChI:InChI=1/C11H16N2O2/c1-8-5-6-12-9(7-8)13-10(14)15-11(2,3)4/h5-7H,1-4H3,(H,12,13,14)

Upstream product

• 695-34-1 2-Amino-4-methylpyridine 
• 24424-99-5 di-tert-butyl dicarbonate 
• 1538-75-6 2,2-dimethylpropanoic anhydride 
• 75-65-0 tert-butyl alcohol 
• 1003-67-4 4-methylpyridine-1-oxide 
• 34619-03-9 di-tert-butyl dicarbonate 
• 501-53-1 benzyl chloroformate 

Downstream Products

• 190189-98-1 (4-bromomethylpyridin-2-yl)carbamic acid tert-butyl ester 
• 308834-68-6 C₂₄H₂₈ClN₇O₂ 
• 677320-17-1 2-(2-t-Butoxycarbonylaminopyridin-4-yl)-1-(3,4-difluorophenyl)ethan-1-one 
• 365427-98-1 tert-butyl {4-[2-(4-fluorophenyl)-2-oxoethyl]-2-pyridyl}carbamate 
• 1207346-17-5 C₁₈H₂₁BrN₂O₂ 
• 1207346-18-6 C₁₈H₂₁BrN₂O₂ 
• 1012305-38-2 2-(N-Boc-N-(1-phenylethyl)amino)-4-methylpyridine 
• 340042-24-2 2-(N-benzyl-N-Boc-amino)-4-methylpyridine 
• 303162-37-0 2-(2-tert-butoxycarbonylamino-pyridin-4-yl)-1-(3-methylphenyl)ethanone 
• 303162-30-3 1-(4-methoxyphenyl)-2-(2-tert-butoxycarbonylamino-pyridin-4-yl)ethanone 
• 475059-57-5 tert-Butyl N-4-[2-hydroxy-2-(4-isopropyl-1,3-thiazol-2-yl)ethyl]-pyridin-2-ylcarbamate 
• 184154-42-5 4-isopropyl-1,3-thiazole-2-carbaldehyde 

Relevant academic research and scientific papers

Catalyst-free synthesis of substituted pyridin-2-yl, quinolin-2-yl, and isoquinolin-1-yl carbamates from the corresponding hetaryl ureas and alcohols

A novel catalyst-free synthesis ofN-pyridin-2-yl,N-quinolin-2-yl, andN-isoquinolin-1-yl carbamates utilizes easily accessibleN-hetaryl ureas and alcohols. The proposed environmentally friendly technique is suitable for the good-to-high yielding synthesis of a wide range ofN-pyridin-2-yl orN-quinolin-2-yl substituted carbamates featuring electron-donating and electron-withdrawing groups in the azine rings and containing various primary, secondary, and even tertiary alkyl substituents at the oxygen atom (48-94%; 31 examples). The DFT calculation and experimental study showed that the reaction proceeds through the intermediate formation of hetaryl isocyanates. The method can be applied to obtainN-isoquinolin-1-yl carbamates, although in lower yields, and ethyl benzo[h]quinolin-2-yl carbamate has also been successfully synthesized (68%).

Mesoionic insecticide

The invention relates to a mesoionic compound. Specifically, the present invention relates to a mesoionic compound represented by formula (I) or a stereoisomer, a nitrogen oxide and a salt thereof ofthe mesoionic compound represented by formula (I), and a process for the preparation of mesoionic compounds, and their use as insecticides in agriculture, and their forms of insecticide compositions,as well as methods of controlling pests with these compounds or compositions; wherein R1, R2, R3, R4, R5, Ra, Rb, Rc, Rd, n, R6 and R7 have the meanings described in the invention.

2-Azo-, 2-diazocine-thiazols and 2-azo-imidazoles as photoswitchable kinase inhibitors: Limitations and pitfalls of the photoswitchable inhibitor approach

In photopharmacology, photoswitchable compounds including azobenzene or other diarylazo moieties exhibit bioactivity against a target protein typically in the slender E-configuration, whereas the rather bulky Z-configuration usually is pharmacologically less potent. Herein we report the design, synthesis and photochemical/inhibitory characterization of new photoswitchable kinase inhibitors targeting p38α MAPK and CK1δ. A well characterized inhibitor scaffold was used to attach arylazo- and diazocine moieties. When the isolated isomers, or the photostationary state (PSS) of isomers, were tested in commonly used in vitro kinase assays, however, only small differences in activity were observed. X-ray analyses of ligand-bound p38α MAPK and CK1δ complexes revealed dynamic conformational adaptations of the protein with respect to both isomers. More importantly, irreversible reduction of the azo group to the corresponding hydrazine was observed. Independent experiments revealed that reducing agents such as DTT (dithiothreitol) and GSH (glutathione) that are typically used for protein stabilization in biological assays were responsible. Two further sources of error are the concentration dependence of the E-Z-switching efficiency and artefacts due to incomplete exclusion of light during testing. Our findings may also apply to a number of previously investigated azobenzene-based photoswitchable inhibitors.

Potent human glutaminyl cyclase inhibitors as potential anti-Alzheimer's agents: Structure-activity relationship study of Arg-mimetic region

Pyroglutamate-modified amyloid β peptides (pGlu-Aβ) are highly neurotoxic and promote the formation of amyloid plaques. The pGlu-Aβ peptides are generated by glutaminyl cyclase (QC), and recent clinical studies indicate that QC represents an alternative t

HETEROARYL RHEB INHIBITORS AND USES THEREOF

The present invention provides compounds, compositions thereof, and methods of using the same. Compositions comprising a compound of this invention or a pharmaceutically acceptable derivative thereof and a pharmaceutically acceptable carrier, adjuvant, or vehicle. The amount of the compound in compositions of this invention is such that it is effective to measurably inhibit Rheb, in a biological sample or in a patient.

KINASE MODULATORS FOR THE TREATMENT OF CANCER

A method of treating cancer in which a compound that inhibits the expression, production or release of IL-10 by immune cells is combined with a compound that stimulates the production of IL-12 when given in combination with, or in the presence of TNFa. Sa

Optimized 4,5-diarylimidazoles as potent/selective inhibitors of Protein Kinase CK1δ and their structural relation to P38α MAPK

The involvement of protein kinase CK1δ in the pathogenesis of severe disorders such as Alzheimer's disease, amyotrophic lateral sclerosis, familial advanced sleep phase syndrome, and cancer has dramatically increased interest in the development of effecti

Discovery of Potent Human Glutaminyl Cyclase Inhibitors as Anti-Alzheimer’s Agents Based on Rational Design

Glutaminyl cyclase (QC) has been implicated in the formation of toxic amyloid plaques by generating the N-terminal pyroglutamate of β-amyloid peptides (pGlu-Aβ) and thus may participate in the pathogenesis of Alzheimer’s disease (AD). We designed a library of glutamyl cyclase (QC) inhibitors based on the proposed binding mode of the preferred substrate, Aβ3E?42. An in vitro structure-activity relationship study identified several excellent QC inhibitors demonstrating 5- to 40-fold increases in potency compared to a known QC inhibitor. When tested in mouse models of AD, compound 212 significantly reduced the brain concentrations of pyroform Aβ and total Aβ and restored cognitive functions. This potent Aβ-lowering effect was achieved by incorporating an additional binding region into our previously established pharmacophoric model, resulting in strong interactions with the carboxylate group of Glu327 in the QC binding site. Our study offers useful insights in designing novel QC inhibitors as a potential treatment option for AD.

Design, synthesis, and evaluation of hinge-binder tethered 1,2,3-triazolylsalicylamide derivatives as Aurora kinase inhibitors

A series of hinge-binder tethered 1,2,3-triazolylsalicylamide derivatives were designed, synthesized, and evaluated for the Aurora kinase inhibitory activities. The novel hinge-binder tethered 1,2,3-triazolylsalicylamide scaffold was effectively assembled by Cu(I)-catalyzed azide-alkyne 1,3-dipolar cycloaddition (CuAAC). A variety of alkynes with hinge binders were used to search proper structures-binding relationship to the hinge region. The synthesized 1,2,3-triazolylsalicylamide derivatives showed significant Aurora kinase inhibitory activity. In particular, 8a inhibited Aurora A kinase with an IC50 value of 0.284 μM, whereas 8m inhibited Aurora B kinase with an IC50 value of 0.364 μM.

The discovery of new cytotoxic pyrazolopyridine derivatives

A number of new 3,7-disubstituted pyrazolo[3,4-c]pyridines have been designed and synthesized from suitable 2-aminopyridines. The antiproliferative activity of the derivatives was determined against the pancreatic MIA PaCa-2 and ovarian SCOV3 cancer cell-lines. IC50values of the most promising analogue 46 lie in the submicromolar or low micromolar range. Furthermore, compound 46 shows similar inhibitory activities against DU145, A2058 and PC-3 cancer cells, blocks the cell cycle at the G0/G1phase and induce apoptosis, as determined by the appearance of apoptotic nuclei.