申请人:Pennwalt Corporation
公开号:US04772705A1
公开(公告)日:1988-09-20
The trans isomeric form of 1,3,4,6,7,11b-hexahydro-7-aryl-2H-pyrazino[2,1-a]isoquinolines are prepared using novel 3-phenyl-4-arylacyl-2-piperazinones and 3-phenyl-4-(2-hydroxy-2-arylethyl) piperazines as intermediates. The process involves reacting a nove piperazinone with a reducing agent such as aluminum hydrides, borane or lithium borohydrides, and then reacting the resulting piperazine with a strong acid, such as polyphosphoric or sulfuric acid.
使用新型的3-苯基-4-芳基酰基-2-哌嗪酮和3-苯基-4-(2-羟基-2-芳基乙基)哌嗪作为中间体,制备了1,3,4,6,7,11b-六氢-7-芳基-2H-吡嗪并[2,1-a]异喹啉的顺式异构体。该过程涉及将新型哌嗪酮与还原剂(如铝氢化物、硼烷或硼氢化锂)反应,然后将得到的哌嗪与强酸(如聚磷酸或硫酸)反应。