342889-39-8

Upstream product

• 1122-91-4 4-bromo-benzaldehyde 
• 94839-07-3 3,4-(methylenedioxy)-benzeneboronic acid 
• 2635-13-4 1,2-(methylenedioxy)-4-bromobenzene 
• 87199-17-5 4-formylphenylboronic acid, 

Downstream Products

• 918799-88-9 N-(4-benzo[1,3]dioxol-5-yl-benzyl)-N-[(methoxy-methyl-carbamoyl)-methyl]-4-pentyl-benzamide 
• 918799-87-8 [(4-benzo[1,3]dioxol-5-yl-benzyl)-(4-pentyl-benzoyl)-amino]-acetic acid methyl ester 
• 918799-89-0 N-(4-benzo[1,3]dioxol-5-yl-benzyl)-N-(2-oxo-ethyl)-4-pentyl-benzamide 

Relevant academic research and scientific papers

Structure-Activity Relationship and Mode-Of-Action Studies Highlight 1-(4-Biphenylylmethyl)-1H-imidazole-Derived Small Molecules as Potent CYP121 Inhibitors

CYP121 of Mycobacterium tuberculosis (Mtb) is an essential target for the development of novel potent drugs against tuberculosis (TB). Besides known antifungal azoles, further compounds of the azole class were recently identified as CYP121 inhibitors with

Palladium nanoparticles supported on carbon nanotubes from solventless preparations: Versatile catalysts for ligand-free Suzuki cross coupling reactions

Palladium nanoparticles supported on single- or multi-walled carbon nanotubes (Pd/SWCNT and Pd/MWCNT) were prepared by a rapid, solventless method that does not require reducing agents or electric current. The method involves a straightforward process using dry mixing of a precursor Pd salt (e.g., palladium acetate) with carbon nanotubes at ambient temperature by ball-milling (mechanochemical route) or with subsequent annealing at 300°C (thermal route) in an inert atmosphere. The Pd/MWCNT sample with Pd nanoparticle size of 1-3 nm and uniform dispersion prepared by mechanochemical ball-milling at room temperature [designated as (Pd/MWCNT)M] displayed remarkable catalytic activity towards Suzuki cross coupling reactions with a high turn over number (TON) of 7250 and turn over frequency (TOF) of 217-500 h-1. These nanoparticles were characterized by a variety of techniques including transmission electron microscopy (TEM), X-ray diffraction (XRD) and X-ray photoelectron spectroscopy (XPS). Additionally, the (Pd/MWCNT)M sample was successfully employed in Suzuki cross coupling reactions with a wide variety of functionalized substrates.

PIPERIDINES USEFUL FOR THE TREATMENT OF CENTRAL NERVOUS SYSTEM DISORDERS

The invention relates to compounds which are substituted chiral or achiral derivatives of 3- or 4- aminopiperidine of the general formula (I). The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more compounds of general formula I and especially their use as inhibitors of β-secretases.

SUBSTITUTED 3- AND 4- AMINOMETHYLPIPERIDINES FOR USE AS BETA-SECRETASE IN THE TREATMENT OF ALZHEIMER’S DISEASE

The invention relates to novel compounds, which are substituted chiral or achiral derivatives of 3- or 4- aminomethylpiperidine of the general formula (I). The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more compounds of general formula (I) and especially their use as inhibitors of beta-secretases for the treatment of Alzheimer’s disease.

Catalyst for aromatic C—O, C—N, and C—C bond formation

The present invention is directed to a transition metal catalyst, comprising a Group 8 metal and a ligand having the structure wherein R, R′ and R″ are organic groups having 1-15 carbon atoms, n=1-5, and m=0-4. The present invention is also directed to a method of forming a compound having an aromatic or vinylic carbon-oxygen, carbon-nitrogen, or carbon-carbon bond using the above catalyst. The catalyst and the method of using the catalyst are advantageous in preparation of compounds under mild conditions of approximately room temperature and pressure.

Air stable, sterically hindered ferrocenyl dialkylphosphines for palladium-catalyzed C-C, C-N, and C-O bond-forming cross-couplings

Pentaphenylferrocenyl di-tert-butylphosphine has been prepared in high yield from a two-step synthetic procedure, and the scope of various cross-coupling processes catalyzed by complexes bearing this ligand has been investigated. This ligand creates a remarkably general palladium catalyst for aryl halide amination and for Suzuki coupling. Turnovers of roughly 1000 were observed for aminations with unactivated aryl bromides or chlorides. In addition, complexes of this ligand catalyzed the formation of selected aryl ethers under mild conditions. The reactions encompassed electron-rich and electron-poor aryl bromides and chlorides. In the presence of catalysts containing this ligand, these aryl halides coupled with acyclic or cyclic secondary alkyl- and arylamines, with primary alkyl- and arylamines, and with aryl- and primary alkylboronic acids. These last couplings provide the first general procedure for reaction of terminal alkylboronic acids with aryl halides without toxic or expensive bases. The ligand not only generates highly active palladium catalysts, but it is air stable in solution and in the solid state. Palladium(0) complexes of this ligand are also air stable as a solid and react only slowly with oxygen in solution.

Application of the fluorous biphase concept to palladium-catalyzed Suzuki couplings

Suzuki C - C couplings were performed in high yields in a fluorous biphase system applying the four differently perfluoro-tagged Pd complexes 2a-d. All four complexes showed similar catalytic activities in the coupling of electron-rich or electron-deficient bromoarenes 3a-e and arylboronic acids 4a-c. Furthermore, we were able to show that all four Pd complexes could be recycled six times without significant decrease in coupling yield. In one example, we were able to reduce the amount of the four catalysts from 1.5 mol-% to 0.1 mol-% in the first runs, but with considerable loss of catalyst activity in repetitive cycles.