摘要
由芳香醛与吗啡啉、氰化钾反应形成的α-芳基-α-(4-吗啡啉)乙腈,可对α,β-不饱合腈或酯进行加成,形成γ-氰基-γ-芳基-γ-(4-吗啡啉)丁酸乙脂。此物与肼缩合得6-取代芳基-4,5-二氢-3(2 H)哒嗪酮,其经芳构化可得6-取代芳基-3(2 H)哒嗪酮。本文报道了7个6-取代芳基-4,5-二氢-3(2 H)哒嗪酮及7个6-取代芳基-3(2 H)哒嗪酮的合成。药理实验表明,其中以2,4-二氯苯基-3(2 H)哒嗪酮的抗惊作用最强,芳环上的取代基对其生物活性具有一定影响。
The α-(aryl)- 4-morpholineacetonitriles obtained from aryl aldehydes, morpholine and potassium cyanide, have been used to synthesize ethyl γ-cyano-γ-(p-chlorophenyl-4-morpholinebutyrate by 1,4-addition to acrylic ester. The above product reacting with hydrazine can yield 6-aryl-4,5-dihydro-3(2H)-pyridazinones in good yields which are dehydrogenated by bromine (via bromination-dehydro-bromination) in acetic acid to give 6-aryl-3(2H)pyridazinones. In searching for effective anticonvulsant agent seven 6 -substituted aryl-4,5-dihydro-3 (2H)pyridazinones and seven 6-substituted aryl-3(2H) pyridazinones have been synthesized and screened. Pharmacological evaluation showed that the anticonvulsant activity (MES) of 2,4-dichlorophenyl--3 (2H) pyridazinone was found to be more potent than other members of the series studied. The substituents on the phenyl ring had some influence for the biological activity too.
出处
《北京医科大学学报》
CSCD
1989年第3期218-220,共3页
Journal of Peking University(Health Sciences)
基金
国家自然科学基金
关键词
抗惊活性
哒嗪类化合物
合成
Anticonvulsant activity 8-aryl-4,5-dihydro-3(2H) pyridazinone 6-aryl-3(2H) pytidazinone
