“…The compounds were dissolved with the help of ethanol, as detailed under the experimental section, that was added to the control runs to eliminate any solvent effect on the aortic strips contractions. We have previously applied the same protocol to evaluate the calcium channel blocking activities of a series of diltiazem-like compounds [17]. The same protocol was also applied in the current research for assessing the activity of the newly designed compounds and the two parent drugs but after incubation for 2-hours, before adding the contractile calcium ions.…”
Section: Evaluation Of Calcium Channel Blocking Activitiesmentioning
“…The compounds were dissolved with the help of ethanol, as detailed under the experimental section, that was added to the control runs to eliminate any solvent effect on the aortic strips contractions. We have previously applied the same protocol to evaluate the calcium channel blocking activities of a series of diltiazem-like compounds [17]. The same protocol was also applied in the current research for assessing the activity of the newly designed compounds and the two parent drugs but after incubation for 2-hours, before adding the contractile calcium ions.…”
Section: Evaluation Of Calcium Channel Blocking Activitiesmentioning
“…The protonation of piperazine is employed as a simple way of protection of the secondary nitrogen atom resulting in the suppression of a competitive reaction leading to disubstituted derivatives. Although the principle of a protonated piperazine was rarely mentioned in literature [26][27][28]32], it was not applied in a broader scale for the synthesis of other monosubstituted piperazines. Nonetheless, our long-time research has shown that the principle is applicable to the synthesis of a wide range of monosubstituted piperazines.…”
Section: One-step Synthesis Of Monosubstituted Piperazine Derivativesmentioning
confidence: 99%
“…In case of some benzyl-and substituted benzyl derivatives, especially fluorinated, above-mentioned issues were suppressed and monosubstituted products were obtained in very high yields [20,[26][27][28][29][30][31][32]. However, the same reaction scheme does not usually work sufficiently well in the case of other substituted benzyl derivatives (yields are usually significantly decreased).…”
We reported a novel simplified synthetic procedure for the preparation of monosubstituted piperazine derivatives which can now be easily prepared in a one-pot-one-step way from a protonated piperazine with no need of introduction of a protecting group. Reactions, proceeding either at room or higher temperatures in common solvents, involve heterogeneous catalysis by metal ions supported on commercial polymeric resins. A general synthetic scheme was successfully applied to afford a wide range of monosubstituted piperazines. Furthermore, we picked up a set of piperazine derivatives and studied the possibilities of microwave acceleration of given synthetic reactions to make them even more efficient. Our research proceeded from a simple batch technique to the construction of a flow microwave reactor prototype and resulted in promising findings which are summarized and discussed in the article.
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