摘要
由芳香醛与吗啡啉、氰化钾反应形成的α-芳基-α-(4-吗啉)乙腈,可对α、β不饱和腈或酯进行1,4-加成,生成1,4-酮酸型化合物。此物与肼缩合,再经芳构化即得6-劳基-3(2H)哒嗪酮。后者再经氯化及氨解可得3-氨基-6-芳基哒嗪。本文应用此法合成了15个3-取代哌嗪-6-取代苯基哒嗪类化合物,并初步测定了它们的抗惊(MES)活性。
The -(aryl) -4- morpholineacetonitriles obtained from aryl aldehydes, morpholine and potassium
cyanide, have been used to synthesize 3-(aroyl) propionic acids and esters by 1,4-additions to acrylon-
itrile or acrylic ester. 3- (aroyl) propionic acids reacting with hydrazine gave 6- aryl-4, 5-dihydro-3
(2H) pyridazinones which were dehydrogenated by bromine (via bromination-dehydrobromination) in
acetic acid to give 6-aryl -3 (2H) pyridazinones. The latter compounds were converted into 3- amino
-6-arylpyridazines by the chlorination (by means of phosphorus oxychloride) and then aminolysis. By
this method fifteen 3-Substituted piperazino-6-(substituted-phe pyridazines were synthseized. The
anticonvulsant activity (MES) of these compounds were also tested.
出处
《北京医科大学学报》
CSCD
1991年第6期477-480,共4页
Journal of Peking University(Health Sciences)
关键词
3-芳酰基丙酸
苯基哒嗪类
衍生物
合成
抗惊厥
3-(aroyl)propionic acid
Phenylpyridazine derivatives
Anticonvulsant activity
