The laboratory synthesis of mazapertine has been reported. It begins with
alkylation of
2-nitrophenol (
1) with
isopropyl bromide to give 2-isopropoxynitrobenzene (
2).
Catalytic hydrogenation of nitro group gives 2-isopropoxyaniline (
3). Intermolecular ring formation of this aniline with bis(2-chloroethyl)amine yields 1-(2-isopropoxyphenyl)piperazine (
4). Separately, amide formation of 3-(chloromethyl)benzoyl chloride (
5) with piperidine gives 1-[3-(chloromethyl)benzoyl]piperidine (
6). The last step is the convergent synthesis between the above two arms of the synthesis to afford the alkylation product mazapertine (
7). : ==References==