A straightforward and efficient method for the synthesis of diversely substituted β-aminoketones and γ-aminoalcohols from 3-(N,N-dimethylamino)propiophenones as starting materials

摘要

Libraries of novel β-aminoketones and γ-aminoalcohols showing a wide structural diversity were easily obtained from a simple approach, using 3-(N,N-dimethylamino)propiophenone derivatives as key starting material. The procedure involved initially an N-alkylation of secondary benzylamines with propiophenone salts yielding the desired β-aminoketones. Chemical or catalytic reduction of their carbonyl groups provided the final γ-aminoalcohols in good yields. This protocol proved to be convenient as an alternative route for the synthesis of the local anesthetic Falicain? and for the topic antifungal drug Naftifine?.