Das B P, Zalkow V B, Forrester M L, Molock F F, Boykin D W
J Pharm Sci. 1982 Apr;71(4):465-6. doi: 10.1002/jps.2600710426.
A series of 1,4-bis(4-guanylphenylethyl)benzenes, including masked amidines in which the guanyl function is incorporated into a heterocyclic ring, were prepared for screening as potential antitrypanosomal agents. Some of these compounds were active against Trypanosoma rhodesiense in mice. The diamidines were prepared by standard methods from 1,4-bis(4-cyanophenylethyl)benzene which was obtained from 1,4-bis(4-cyanostyryl)benzene by diimide reduction. The latter compound was prepared by the Wittig reaction between 4-cyanobenzylphosphonium ylide and terephthaldicarboxaldehyde.
制备了一系列1,4 - 双（4 - 胍基苯乙基）苯，包括胍基官能团并入杂环的掩蔽脒，以筛选潜在的抗锥虫剂。其中一些化合物对小鼠体内的罗德西亚锥虫具有活性。二脒是通过标准方法由1,4 - 双（4 - 氰基苯乙基）苯制备的，而1,4 - 双（4 - 氰基苯乙基）苯是由1,4 - 双（4 - 氰基苯乙烯基）苯经二亚胺还原得到的。后一种化合物是通过4 - 氰基苄基鏻叶立德与对苯二甲醛之间的维蒂希反应制备的。
