82292-39-5Relevant academic research and scientific papers
IMPROVED METHOD FOR THE PRODUCTION OF N-SUBSTITUTED AMIDES FROM NITRILES
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Page/Page column 10, (2010/02/06)
An improved method for the production of N-substituted amides of formula RCONHR1 (I) wherein R represents an optionally monosubstituted or polysubstituted C1-C20-alkyl-, C5 -C20-aryl- or C5-C20--heterocyclic radical and R1 represents an optionally monosubstituted or polysubstituted C1-C20-alkyl- or C5-C20-aryl radical from corresponding nitriles of formula RCN (II) wherein R1 is defined as above, wherein a nitril of formula (II) is reacted in polyphosphoric acid with an alcohol of formula R10H (III) wherein R1 is as defined above, in the presence of a compound from the group consisting of phosphorpentoxide, phosphoroxychloride, sulfurylchloride, dialkylcarbonate and dialkylsulfate at a temperature of 80 -190 °C to form the corresponding N-substituted amide.
Aromatic analogs of arcaine inhibit MK-801 binding to the NMDA receptor
Sharma, Terre A.,Carr, Andrew J.,Davis, Rebecca S.,Reynolds, Ian J.,Hamilton, Andrew D.
, p. 3459 - 3464 (2007/10/03)
Aromatic analogs of arcaine were shown to have inhibitory effects on the binding of the channel blocking drug [3H]MK-801 to the NMDA receptor complex. The most potent compound of the series was an N,N - bis(propyl)guanidinium which inhibited [3H]MK-801 binding with an IC50 of 0.58 μM and an IC50 of 12.17 μM upon addition of 100 μM spermidine. The increase in IC50 upon addition of spermidine suggests competitive antagonism between the inhibitor and spermidine at the arcaine-sensitive polyamine site of the NMDA receptor complex.
