Abstract2‐Benzoyl‐ and 2‐(2‐naphthoyl)pyrrolidines which can be viewed asarylα‐amino ketones, have been prepared from L‐proline via Grignard reactions, bromo‐to‐lithium exchange, or by Friedel‐Crafts acylations. It was impossible to convert the ketone function of thesearylα‐amino ketones into atert‐alcohol group. The BOC‐protected (S)‐2‐acetyl‐l‐pyrrolidine (15), obtained by reaction of BOC‐proline 2‐pyridinethiol ester (2) with LiMe2Cu, could be converted in two steps into the amino alcohol17, which contains atert‐alcohol function. Upon treatment of17with BBr3, followed by air oxidation, mitosene20was obtained in a low yield. The Friedel‐Crafts reaction products23of 1,4‐dimethoxynaphthalene, or 2,5‐dimethoxytoluene and (S)‐l‐(trifluoroacetyl)–2‐pyrrolidinecarbonyl chloride, could be converted in two steps into theisomitosanes25. The isomitosanes25could easily be dehydrated, using acid, to the corresponding mitosenes26. Upon reduction of the isomitosanes25with Na2S,2O4to the correspond