SYNTHESIS OF 2-SUBSTITUTED-DITHIOFORMIC ACID ESTER ANALOGUES OF ANTISCHISTOSOMAL DRUG PRAZIQUANTEL. [J]. Journal of Chongqing Medical University (4):306-308(1988)
SYNTHESIS OF 2-SUBSTITUTED-DITHIOFORMIC ACID ESTER ANALOGUES OF ANTISCHISTOSOMAL DRUG PRAZIQUANTEL. [J]. Journal of Chongqing Medical University (4):306-308(1988) DOI: 10.13406/j.cnki.cyxb.1988.04.023.
SYNTHESIS OF 2-SUBSTITUTED-DITHIOFORMIC ACID ESTER ANALOGUES OF ANTISCHISTOSOMAL DRUG PRAZIQUANTEL
摘要
为寻找抗血吸虫病新药
对吡喹酮的化学结构进行修饰
合成了五种新的吡喹酮类似物:2-二硫代甲酸酯-1:2
3
6
7
11b-六氢-4H-吡嗪并[2
1-a] 异喹啉-4-酮
动物实验筛选的结果表明化合物Vla、c、e治疗感染小鼠后的减虫率在10%左右
抗血吸虫作用较吡喹酮差.中间体2-苯甲酰基-1
2
3
6
7
11b-六氢-4H-吡嗪并[2
1-a]异喹啉-4-酮的合成
采用相转移法
避免了原环合反应中的缺点.
Abstract
In order to obtain antischistosomal agents by modification of the chemical structure of praziquantel
five compounds of 2-substituted dithioformic acid ester of 1
2
3
6
7
11b-hexahydro-4H-pyrazine [2
1-a] isoquinolinones Were synthesized.Screening with experimental
compound VIa
c and e showed lower activity against schistosomiasis japonicum in mice than praziquantel.2-Benzoyl-1
2
3
6
7
11b-hexahydro-4H-pyrazine [2
1-a] iscquinolin-4-ones
a key intermediate for the synthesis of praziquantel analogues
was prepared by utilizing phase transfer catalysis techniques in 86% yield from 1-benzoylaminomethyl- -chloroacetyl-1