N-取代-3-卤代-2,4,6-三甲苯胺类化合物的合成
CHEMOTHERAPY OF SCHISTOSOMIASIS Ⅰ.SYNTHESIS OF N-SUBSTITUTED-3-HALO-MESIDINES
-
摘要: 本文报告了9种N-取代-3-卤代-2,4,6-三甲苯胺类化合物的合成.它们用作日本血吸虫病的动物治疗突验.这类化合物是由三甲苯用发烟硝酸行二硝基化成2,4-二硝基1,3,5-三甲苯,用硫化钠及硫还原一个硝基得3-硝基-2,4,6-三甲苯胺,重氮化接上卤素,再用铁屑还原得3-卤代-2,4,6-三甲苯胺,再与N-取代β-氯乙基胺在硝基苯中缩合而得N-取代-3-卤代-2,4,6-三甲苯胺类化合物.Abstract: Nine N-substituted-3-halo-mesidines have been synthesized for the purpose of testing their activities against Schistosomiasis japonica in experimentally infected animals. They were synthesized by the condensation of 3-halo-mesidines with substituted aminoethyl chloride.The 3-halogenated mesidines were obtained from mesitylene via nuclear dinitration,partial reduction to nitro-amines,diazotization to introduce a halogen group,and reduction of the remaining itro group. The halogenated mesidines synthesized by the above route were of superior yield to those ob- tained by other methods such as monohalogenation,nitration,and reduction,or mononitration, reduction,and direct halogenation.
下载: