3-取代哌嗪-6-取代苯基哒嗪的合成及抗惊活性的研究  

STUDIES ON SYNTHESIS AND ANTICONVULSANT ACTIVITY OF 3-SUBSTITUTED PIPERAZINO -6-(SUBSTITUTED-PHENYL) PYRIDAZINES

作　　者：徐萍[1] 王书玉[1] 梁鸿[1] 张春桃 刘维勤[1] 

机构地区：[1]北京医科大学药学院

出　　处：《北京医科大学学报》1991年第6期477-480,共4页Journal of Peking University(Health Sciences)

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.

关 键 词：3-芳酰基丙酸 苯基哒嗪类 衍生物 合成 抗惊厥 

分 类 号：R971[医药卫生—药品]