申请人:Michel Dominique
公开号:US20110004007A1
公开(公告)日:2011-01-06
A process is disclosed for the preparation of a compound of formula
and/or an addition salt of a proton acid, wherein R
1
and R
2
independently represent alkyl, cycloalkyl, aryl or aralkyl, each aryl or aralkyl being optionally further substituted with alkyl, alkoxy and/or halogen. The process involves reacting a mixture comprising a methyl ketone of formula
and a compound of formula H
2
N—R
2
(V) and/or an addition salt of proton acid, and formaldehyde in the presence of a solvent selected from the group consisting of water, aliphatic alcohols, cycloaliphatic alcohols and mixtures thereof, and optionally a proton acid to afford a β-amino ketone of formula
and/or an addition salt of a proton acid, and reducing the carbonyl group of said β-amino ketone to afford a compound of formula I, and/or an addition salt of a proton acid
wherein the first step is carried out at a pressure above 1.5 bar.
本发明公开了一种制备式(I)化合物和/或质子酸加合盐的方法,其中R1和R2分别独立地表示烷基,环烷基,芳基或芳基烷基,每个芳基或芳基烷基可以选择进一步取代烷基,烷氧基和/或卤素。该方法包括在水,脂肪醇,环烷醇和其混合物中选择的溶剂存在下,通过反应式为甲基酮和式为H2N-R2(V)和/或质子酸加合盐的混合物以及甲醛来制备β-氨基酮化合物和/或质子酸加合盐,然后还原所述β-氨基酮的羰基基团以制备式I化合物和/或质子酸加合盐,其中第一步在大于1.5巴的压力下进行。