化学学报 ›› 1964, Vol. 30 ›› Issue (2): 146-152. 上一篇    下一篇

论文

降压药物的合成研究Ⅱ.若干氮七环基和氮八环基化合物的合成

白东鲁, 嵇汝运   

  1. 中国科学院药物研究所
  • 投稿日期:1963-05-13 发布日期:2013-06-03

SYNTHETIC STUDIES ON HYPOTENSIVE AGENTS Ⅱ. THE PREPARATION OF SOME COMPOUNDS CARRYING HEXAMETHY-LENIMINO AND HEPTAMETHYLENIMINO GROUPS

BAI DONG-LU, KYI ZU-YOONG   

  1. Institute of Materia Medica, Academia Sinica
  • Received:1963-05-13 Published:2013-06-03

1-邻氯苄基氮七环和1-邻氯苄基氮八环与碘乙烷、邻氯苄基溴或对甲苯磺酸甲酯分别反应,生成相应的季铵盐(Ⅲa,b,c,e);N,N-环六亚甲基-N',N'-环七亚甲基-1,2-乙二胺与邻氯苄基溴反应,得到双季铵盐(Ⅲd).1-β-氯乙基氮七环和1-β-氯乙基氮八环与过量的水合肼或氮八环作用,各自得β-取代氨基乙肼(Ⅳa,b)和1,2-乙二胺化合物(Ⅳf).水合肼与1-氮七环基乙醛缩合,生成的连氮化合物用氢化铝锂还原得N,N'-双-(β-1-氮七环基乙基)肼(Ⅳc).由1,2-二溴乙烷与氮七环或氮八环反应,得对称乙二胺衍生物(Ⅳd,e).借1-β-氯乙基氮七环双分子环合季铵化和1,2-乙二胺衍生物与二溴代烷的反应,得螺环双季铵盐(Ⅳ).

Bretylium (Ⅰ) and guanethidine (Ⅱ) were reported to have protracted antihypertensive properties with the capacity to block the transmission at peripheral adrenergic nerve terminals.It appears interesting to study the relationship between their chemical constitutions and pharmacological activities.The present work deals with the structural modification of Ⅰ and Ⅱ.