This 1-alkoxyphthalan alcohol (CIV) then has the hydroxyl group converted into a leaving group such as mesylate, tosylate, or halides (X2 =--OMs, --OTs, --Cl, --Br, or --I) to give the 1-alkoxyphthalan derivative (CV), which is then coupled with R2 --Ar/Het (LXV) using diisopropylethylamine as the base and refluxing in ethylene glycol, to give the desired 1-alkoxyphthalan-3-ethylene amine (CIII).