Synthesis of <i>N</i>-(2-(Methylamino)ethyl) Derivatives of 2<i>H</i>-Phthalazin-1-ones

<div><p></p><p>A series of new alkyl, tosyl, acetyl, and <i>tert</i>-butoxycarbonyl derivatives of 2-(2-aminoethyl)-phthalazinones were efficiently synthesized by reaction of lactams with <i>N</i>-Boc-, <i>N</i>-acetyl-, or <i>N,O</i>-ditosyl derivatives of <i>N</i>-methylethanolamine in the presence of MeONa or under Mitsunobu reaction conditions. Selected compounds were converted into corresponding 2-[2-(methylamino)ethyl]phthalazinones in good yields.</p> </div>