169883-33-4

Upstream product

• 104-10-9 2-(4'-aminophenyl)ethyl alcohol 
• 75178-16-4 2-(4-Acetamidophenyl)ethyl acetate 
• 100-27-6 2-(4-nitrophenyl)ethanol 

Downstream Products

• 1431943-60-0 2-bromo-4-(2-{2-oxo-4-[2-(1-oxo-1,3-dihydro-2-benzofuran-5-yl)ethyl]piperazin-1-yl}ethyl)benzonitrile 
• 1374357-67-1 2-bromo-4-(2-oxoethyl)benzonitrile 
• 1431944-08-9 tert-butyl (2-{[2-(3-bromo-4-cyanophenyl)ethyl]amino}ethyl)carbamate 
• 1431944-09-0 tert-butyl (2-{[2-(3-bromo-4-cyanophenyl)ethyl](chloroacetyl)amino}ethyl)carbamate 
• 1431944-07-8 2-bromo-4-[2-(2-oxopiperazin-1-yl)ethyl]benzonitrile 
• 1374358-11-8 2-bromo-4-(2-hydroxyethyl)benzonitrile 
• 949495-46-9 2-amino-5-(2-hydroxyethyl)benzonitrile 
• 915006-20-1 2-(4-amino-3-cyclohex-1-enyl-phenyl)-ethanol 
• 1420011-82-0 C₂₅H₄₀BrNO₂Si 
• 1420009-32-0 C₂₇H₃₁NO₃ 
• 1420012-09-4 C₂₇H₄₄BrNO₂Si 
• 1420012-02-7 C₂₃H₃₄BrNO₃Si 

Relevant academic research and scientific papers

SUBSTITUTED QUINAZOLINONE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR4

The present invention relates to novel quinazolinone derivatives of formula (I) as well as pharmaceutical compositions containing these compounds. The compounds of formula (I) as provided herein can act as positive allosteric modulators of metabotropic glutamate receptor subtype 4 (mGluR4), and can thus be used as therapeutic agents, particularly in the treatment or prevention of conditions associated with altered glutamatergic signalling and/or functions or conditions which can be affected by alteration of glutamate level or signalling.

SUBSTITUTED INDOLE MCL-1 INHIBITORS

The present disclosure provides for compounds that inhibit the activity of an anti- apoptotic Bcl-2 family member Myeloid cell leukemia-1 (Mcl-1) protein. The present disclosure also provides for pharmaceutical compositions as well as methods for using co

A Pd(0)-mediated indole (macro)cyclization reaction

Herein we report a systematic study of the Larock indole annulation designed to explore the scope and define the generality of its use in macrocyclization reactions, its use in directly accessing the chloropeptin I versus II DEF ring system as well as key

INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL

The present invention provides compounds of Formula (I) and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir 1.1) channel. The compounds act as diuretics and natriuretics and are valuable pharmaceutically active compounds for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension and conditions resulting from excessive salt and water retention.

Enhancement of kinase selectivity in a potent class of arylamide FMS inhibitors

Structure-activity relationship (SAR) studies on a highly potent series of arylamide FMS inhibitors were carried out with the aim of improving FMS kinase selectivity, particularly over KIT. Potent compound 17r (FMS IC50 0.7 nM, FMS cell IC50 6.1 nM) was discovered that had good PK properties and a greater than fivefold improvement in selectivity for FMS over KIT kinase in a cellular assay relative to the previously reported clinical candidate 4. This improved selectivity was manifested in vivo by no observed decrease in circulating reticulocytes, a measure of bone safety, at the highest studied dose. Compound 17r was highly active in a mouse pharmacodynamic model and demonstrated disease-modifying effects in a dose-dependent manner in a strep cell wall-induced arthritis model of rheumatoid arthritis in rats.

Design, synthesis, and biological evaluation of Plasmodium falciparum lactate dehydrogenase inhibitors

Plasmodium falciparum lactate dehydrogenase (pfLDH) is a key enzyme for energy generation of malarial parasites and is a potential antimalarial chemotherapeutic target. It is known that the oxamate moiety, a pyruvate analog, alone shows higher inhibition

C-FMS KINASE INHIBITORS

The invention is directed to compounds of Formula II: wherein A, R1, R2, R3, R4, X, Y and W are set forth in the specification, as well as solvates, hydrates, tautomers or pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase.

1N-ALKYL-N-ARYLPYRIMIDINAMINES AND DERIVATIVES THEREOF

The present invention provides novel compounds, compounds and pharmaceutical compositions thereof, and methods of using same in the treatment of affective disorders, anxiety, depression, post-traumatic stress disorders, eating disorders, supranuclear palsy, irritable bowel syndrome, immune suppression, Alzheimer'disease, gastrointestinal diseases, anorexia nervosa, drug and alcohol withdrawal symptoms, drug addiction, inflammatory disorders, or fertility problems. The novel compounds provided by this invention are those of formula: wherein R 1, R 3, R 4, R 5, Z, Y, V, X, X', J, K, L, and M are as defined herein.

Total synthesis of vancomycin - Part 1: Design and development of methodology

o-Halosubstituted aromatic triazenes (e.g. I, Scheme 1) react with aryloxides (e.g. II, Scheme 1) in the presence of CuBr · Me2S, K2CO3 and pyridine in acetonitrile at reflux to afford biaryl ethers (e.g. V, Scheme 1). This general methodology (Tables 1 and 2) was applied to the construction of the C-O-D and D-O-E vancomycin model systems 37 (Scheme 2) and 50 (Scheme 3), demonstrating its potential in a projected total synthesis of vancomycin (1. Figure 1). For the construction of the vancomycin model AB biaryl ring system, a sequential strategy involving a Suzuki coupling of the C-O-D aryl iodide 74 (Scheme 7) and boronic acid 53 (Scheme 4), followed by macrolactamization was demonstrated, in which the preformed C-O-D ring framework served to preorganize the precursor for cyclization. The latter investigation led to Suzuki-coupling-based asymmetric synthesis of biaryl systems in which 2,2-bis(diphenylphosphino)-1,1'-binaphthyl (BINAP) was found to be the optimum ligand (Tables 3 and 4).

A Suzuki coupling-macrolactamization approach to the AB-COD bicyclic system of vancomycin

The effectiveness of the Suzuki coupling reaction in the formation of the AB biaryl moiety and the beneficial role of a preexisting COD ring system in a lactamization approach to the AB-COD ring system of vancomycin is demonstrated.