This work is focused on the electrochemical late-stage modification of hydralazine (1-hydrazinylphthalazine) (HYD), a commonantihypertensive drug, and the synthesis of its new sulfonylhydrazine derivatives. The synthe sis of HYD derivatives has been easily accomplished in one-pot via electrochemical oxidation of HYD in the pres ence of arylsulfinic acid derivatives (ASA) in a water/ethanol mixture at constant current conditions. The electro chemical results show that anodically generated 1-diazenylphthalazine (HYDox) reacts with arylsulfinic acids and converts into the corresponding sulfonylhydrazine derivatives (SHD) with high yield and purity in an undi vided cell equipped with graphite anode and stainless steel cathode. The main feature of this work is the synthe sis of some new HYD derivatives in water/ethanol mixture as a “Green” reaction medium, using electrodes in stead of toxic oxidants, having a high atom economy, having good energy efficiency and working at room tem perature. These features are in accordance with the principles of green chemistry. Another advantage of this ap proach is that this method has led to the synthesis of sulfonylhydrazine derivatives in nano dimensions. Also, in this work, the electrochemical behavior of HYD and synthesized compounds (SHD) by different electrochemical methods were fully investigated and the results were reported. Furthermore, docking studies suggest that the products interact well with arylamine N-acetyltransferase (NAT) and show promising activity.
