A scaleable synthetic route is described to obtain 2-(4-acetylpiperadin-1-yl)-6-[3,5-bis(trifluoromethyl)phenylmethyl]-4-(2-methylphenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-b][1,5]oxazocin-5-one (1, KRP-103) as a neurokinin (NK)(1) antagonist. The key step in the synthesis is the intramolecular cyclization of N-[3,5-bis(trifluoromethyl)phenylmethyl]-N-(3-hydroxypropyl)-4-chloro-6-(2-methylpheny...

the reaction of copper(ii) chloride and zinc(ii) chloride with n-(2-methylphenyl)-3-(1'-salicylaldehydene-2'-imine-ethane)-butanamide(h2l2a) or (mpsb), n-(2-methylphenyl)-3-(1'-(3'-methoxysalicylaldehydene-2'-imine-ethane)-butanamide (h2l2b) or (mpmsb) and n-(2-methylphenyl)-3-(1'-(2'-hydroxyacetylene-2'-imine-ethane)-butanamide (h2l2c) (mphb) leads to th...

Background and Objective: Regarding the prevalence of epilepsy in human society and with respect to insufficiency of usual treatments, new strategies and methods for medical treatment of epileptic patients are necessary. As NMDA receptor antagonists are the most prominent anti-epileptic drugs, in the present study, we synthesized and investigated anti-epileptic effect of a new piperidine deriva...

A decalin gel consisting of a 3,3'-bis[{(octylamino)carbonyl}propoxy]azobenzene derivative with H-aggregation showed a photon-density dependent E-Z isomerization, indicating the cooperating isomerization of each module.

The potential of selected microorganisms to O-dealkylate alkyl aryl ethers in a manner analogous to mammalian systems has been studied. A total of 45 fungi and actinomycetes were screened for their ability to O-demethylate 4-methoxybiphenyl. Of the 20 organisms found to actively metabolize this substrate, 5 were chosen for additional study. Incubation with a series of five homologous 4-alkoxybi...

Transient precursor states are often experimentally observed for molecules adsorbing on surfaces. However, such precursor states are typically rather short-lived, quickly yielding to more stable adsorption configurations. Here we employ first-principles calculations to systematically explore the interaction mechanism for benzene derivatives on metal surfaces, enabling us to selectively tune the...

The reactions of distonic 4-(N,N,N-trimethylammonium)-2-methylphenyl and 5-(N,N,N-trimethylammonium)-2-methylphenyl radical cations (m/z 149) with O2 are studied in the gas phase using ion-trap mass spectrometry. Photodissociation (PD) of halogenated precursors gives rise to the target distonic charge-tagged methylphenyl radical whereas collision-induced dissociation (CID) is found to produce u...

Enantioselective hydrolysis of bromo- and methoxy-substituted 1-phenylethanol acetates was conducted using comminuted carrot (Daucus carota L.) and celeriac (Apium graveolens L. var. rapaceum) roots. Hydrolysis of the acetates led to alcohols, preferentially to R-(+)-enantiomers. Efficiencies of both reactions - hydrolysis of the acetates with an electron-donating methoxy group and oxidation of...

An< accurate, stable and very fast corner finder (for feature based vision) has been developed', based on a novel definition of corners, using:no image derivatives. This note describes the algorithm and the results obtained from its use.