The invention is concerned with a process for the preparation of a benzo[a]quinolizinone derivative of the formula ##STR1## by reacting a compound of the formula ##STR2## wherein X is halogen and Ph is phenyl, with carbon monoxide in the presence of a carbonylation catalyst and in the presence of (S)-3-ethoxypyrrolidine or a lower alkanol or water; where a lower alkyl ester of the 10-chloro-6,7-dihydro-4-oxo-3 -phenyl-4H-benzo[a]quinolizine-1-carboxylic acid has been obtained, converting this into the corresponding free acid; and, where the 10-chloro-6,7-dihydro-4-oxo-3-phenyl-4H-benzo[a]quinolizine-1-carboxylic acid has been obtained, reacting a reactive derivative thereof with (S)-3-ethoxypyrrolidine. The compound of formula I is useful for the treatment or prophylaxis of sleep disorders.
本发明涉及一种制备公式为##STR1##的苯并[a]喹诺利酮衍
生物的方法,该方法通过在羰基化催化剂和(S)-3-乙氧
吡咯烷或较低的烷醇或
水的存在下,将公式为##STR2##的化合物(其中X是卤素,Ph是苯基)与
一氧化碳反应而得到。其中,已获得10-
氯-6,7-二氢-4-氧代-3-苯基-4H-苯并[a]喹诺利啉-1-
羧酸的较低烷基酯,将其转化为相应的自由酸;已获得10-
氯-6,7-二氢-4-氧代-3-苯基-4H-苯并[a]喹诺利啉-1-
羧酸的反应性衍
生物,与(S)-3-乙氧
吡咯烷反应。公式I的化合物可用于治疗或预防睡眠障碍。