科研之友
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摘要
Libraries of novel beta-aminoketones and gamma-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 beta-aminoketones. Chemical or catalytic reduction of their carbonyl groups provided the final gamma-aminoalcohols in good yields. This protocol proved to be convenient as an alternative route for the synthesis of the local anesthetic Falicain (R) and for the topic antifungal drug Naftifine (R).
- 出版日期2013-9
