The synthesis and biological activity of new 7‐[2‐(cyanomethyl)piperazinyl]‐ and 7‐[3‐(cyanomethyl)piperazinyl]quinolone antibacterials

Abstract

Abstract Some novel 7‐[2‐ or 3‐(cyanomethyl)piperazinyl]quinolones have been prepared. Most notable, 2‐cyanomethyl‐piperazine 5 and 1‐methyl‐2‐cyanomethylpiperazine 8 at the quinolone C‐7 position produce products with good in vitro antibacterial activity. The key step in the synthesis of these products involves the regioselective deprotection of the benzyl group in function of the time reaction.