NIS-Catalyzed Reactions: Amidation of Acetophenones and Oxidative Amination of Propiophenones

Single-step amination: The N-iodosuccinimide (NIS)-catalyzed amidation of acetophenone derivatives by using tert-butylhydroperoxide (TBHP) as an oxidant is presented. A variety of acetyl derivatives of heterocyclic compounds were easily converted to their corresponding ketoamides under these conditions. A new, NIS-catalyzed amination of propiophenone and its derivatives in the presence of TBHP to furnish the corresponding 2-aminoketone derivatives is the first reported single-step amination of propiophenone derivatives.

Modificacoes na ação mecânica do coração isolado de cobaia por doses de propafenon capazes de alterar o eletrocardiograma

Inotropic effects of Propafenon were studied in isovolumic isolated guinea pig hearts submitted to infusion of the drug during 10 minutes. The dosages utilized caused: bradycardia, depression of AV nodal conduction and QRS widening. Simultaneously there was: decrease of the developed pressure (DP) and of the rate of rise of pressure (dp/dt), and elongation of the time of peak pressure. Since there was no clear relation between the heart rate and the inotropic indices (PD and dp/dt), it could be supposed that the depressor effect was not due to impairment of the chronotropism only. After the infusion of Propafenon, the chronotropic effect disapeared after 15 min, while the inotropic state presented a less satisfatory recuperation. The coronary output accompanied the myocardial metabolic needs, that is to say, there was a fall during the period of depressed cardiac function and a later tendency to increase during recovery.