Phosphinyl analogues of hydroxybupropion: (±)-2-aryl-3,3,5,5-tetramethyl-[1,4,2]-oxazaphosphinanes

Analogous structures in phosphinate series of hydroxybupropion 2, that is, (±)-2-aryl-3,3,5,5-tetramethyl-[1,4,2]-oxazaphosphinanes 8, are prepared according to a two step sequence: addition–cyclization reaction from methyl hypophosphite and oxazolidine 6, followed by a pallado-catalyzed arylation of P–H bond from oxazaphosphinane 7.