1,7-双[2-二烃氦甲基-4-替代基-苯氧基]庚烷衍生物的合成

本文报导合成了1,7-双-2-二烃氨甲基-4-替代基苯氧基]-庚烷衍生物七种,其中除1,7-双-2-二乙氨甲基-4-氨基苯氧基]庚烷,由1,7-双-2-二乙氨甲基-4-乙酰氨基苯氧基]庚烷水解制得外,其它均由相应的苯酚与1,7-二溴庚烷作用制取。制备苯酚类时的Mannich反应,系采用双-(二經氨基)甲烷为試剂。

SYNTHESIS OF 1,7-BIS-(2-DIALKYLAMINOMETHYL-4-SUBSTI TU-TED-PHENOXY)-HEPTANES

Seven new compounds, 1,7-bis-(2-dialkylaminomethyl-4-substituted-phenoxy)-heptanes, have been prepared from 1,7-dibromoheptane and 2-dialkylaminomethyl-4-substituted-phenols in the presence of potassium hydroxide. By using this method, 1,7-bis-(pnitrophenoxy)-heptane was obtained instead of the expected 1,7-bis-(2-dialkylaminomethyl-4-nitrophenoxy) heptane. The 1,7-bis (2-diethylaminomethyl-4-aminophenoxy)-heptane was formed by hydrolysis of the corresponding acetyl derivative. The bis-(dialkylamino)-methanes were adopted as Mannish reagents to react with 4-substitued-phenols. The yield of 2-diethylaminomethyl-4-nitrophenol is 73-75%. The above new compounds are to be tested for the activity against Schistosomiasis Japonica in experimentally infected animals. The results will be published elsewhere.