Conditions have been developed for the palladium-catalyzed cross-coupling of 3-bromo-2,1-borazaronaphthalenes with potassium alkenyltrifluoroborates. Twenty-seven alkenyl-substituted azaborines have been synthesized through this method, providing access to a family of 2,1-borazaronaphthalenes with alkenyl substitution at the C3 position.

A general method for the alkenylation of alkyl electrophiles using nearly stoichiometric amounts of the air- and moisture-stable potassium organotrifluoroborates has been developed. Various functional groups were tolerated on both the nucleophilic and electrophilic partner. Reactions of highly substituted E- and Z-alkenyltrifluoroborates, as well as vinyl- and propenyltrifluoroborates, were suc...

ATP-sensitive potassium (KATP) channel openers have a relaxation effect due to the lower cellular membrane potential and inhibit calcium influx. There has been considerable interest in exploring KATP channel openers in the treatment of various diseases such as cardiovascular, cerebrovascular, and urinary system disease and premature labor. The purpose of this study was to synthesize 3,3,6,6-tet...

Demyelinating diseases like multiple sclerosis (MS) uncover internodal potassium channels in myelinated axons (Chiu and Ritchie 1982), thus rendering impulse propagation difficult (Waxman 1987). Therefore, the role of potassium channel blockers like 4-aminopyridine (Stefoski et al. 1991; van Diemen et al. 1991) and substituted benzofurans (Bohuslavizki et al. 1993) in the symptomatic treatment ...

The present study reports a microwave-assisted method for the synthesis of twelve novel tricyclic 1,4-dihydropyridine derivatives in which dimethyl-substituted cyclohexane and / or tetrahydrothiophene rings are fused to the DHP ring. The structures of the compounds were confirmed by spectral methods and elemental analysis. The potassium channel opening effects of the compounds were determined o...

A series of substituted aliphatic nitriles have been trimerized to their corresponding pyrimidine structures under solvent-free conditions in the presence of catalytic quantities of potassium tert-butoxide using a focused microwave reactor. Multigram quantities of the corresponding 4-aminopyrimidines have been prepared in high yields and purity following a simple and scaleable protocol.

Ethyl (3-methyl-7-substituted-2-oxoquinoxalin-1(2H)-yl) acetates 2a-c are prepared by the condensation of ethyl chloroacetate with 3-methyl-7-substituted quinoxalin-2(1H)-ones 1a-c. The reaction of 2a-c with hydrazine hydrate furnished 2-(3-methyl-7-substituted-2-oxoquinoxalin-1(2H)-yl) acetohydrazides 3a-c, which on cyclisation with substituted aromatic carboxylic acids in the presence of phos...

To assess the application potential of novel biomaterials, their behaviour in model media and upon sterilization should be investigated, as well stability related to storage conditions. Such data are lacking for Mg-substituted HAP (Mg-HAP). Therefore, changes local structure non-substituted Mg-HAP after irradiation immersion corrected simulated fluid saline solution 28 days were followed by ele...