Synthesis of optically pure a-tert-butyl 0-methyl (2S,3R)-3-ethylhexahydroquinolinate (18) in 54-59% yield from L-aspartic acid was the foundation for a practical synthesis of (+)-vincamine. Conversion of L-aspartic acid to 18 was accomplished via two routes. In the first route, esterification was followed by mono-N-alkylation to attach the three-carbon residue. Nitrogen protection and intramol...

An integrated process coupling solid-liquid extraction and liquid-membrane preconcentration of vincamine was studied. The effect of the ratios solid phase/extractant volume and extractant volume/liquid membrane volume on the mass transfer rate and efficiency of vincamine removal were estimated. It was found that the transfer rate and removal efficiency of the alkaloid were higher with smaller q...

Description Vinpocetine (vinpocetine-ethyl apovincaminate) was synthesized in the late 1960s from the alkaloid vincamine, extracted from the leaf of the lesser periwinkle plant (Vinca minor). Vinpocetine was made available under the trade name Cavinton in 1978 and has since been used widely in Japan, Hungary, Germany, Poland, and Russia for the treatment of cerebrovascular-related pathologies. ...

Vinpocetine, a synthetic derivative of the Vinca minor alkaloid vincamine, is a widely used drug in neurological practice. We tested the hypothesis that vinpocetine binds to peripheral benzodiazepine binding sites (PBBS) and is therefore a potential ligand of PBBS. Positron emission tomography (PET) measurements in two cynomolgous monkeys showed that pretreatment with vinpocetine markedly reduc...

Mucin overproduction is a hallmark of otitis media (OM). Streptococcus pneumoniae is one of the most common bacterial pathogens causing OM. Mucin MUC5AC plays an important role in mucociliary clearance of bacterial pathogens. However, if uncontrolled, excessive mucus contributes significantly to conductive hearing loss. Currently, there is a lack of effective therapeutic agents that suppress mu...

periwinkle (vinca minor l.) is an evergreen perennial herbaceous plant that belongs to the family apocynaceae. the aerial part of this plant contains certain alkaloids such as vincamine, isovincamine and vincine. the most important of these is vincamine that re-duces blood pressure and promotes memory and the ability for mental concentration. mi-cropropagation could be a good alternative for th...

In the current study, a number of alkaloids including retamine, cytisine, and sparteine (quinolizidine-type), yohimbine and vincamine (indole-type), scopolamine and atropine (tropane-type), colchicine (tropolone-type), allantoin (imidazolidine-type), trigonelline (pyridine-type) as well as octopamine, synephrine, and capsaicin (exocyclic amine-type) were tested in vitro for their inhibitory act...