【摘要】 本文介绍由α-溴代苯乙酸乙酯经五步反应合成了4-(N,N-取代氨基烷基)-2-苯基(或对氯苯基)-硫代吗咻Ⅲ,它与有较好辐射防护效果的药物氯丙嗪及对氯苯乙胺结构有相似之处。经药理试验结果,化合物Ⅲ_d。在Ⅹ-射线600伦照射后,对小白鼠的急性放射病有一定防护效果。更多还原

【Abstract】 In our early work, it was shown that p-chlorophenylethylamine and chloropromazine exhibited remarkable protective effect against ionization radiation in mice. The prophylactic mechanisms of these drugs were quite different from that of mercaptoethylamine. Accordingly, synthesis of compounds structurally related to both p-chlorophenylethylamine and chloropromazine would be interesting in search for antiradiation drugs.N-amino-alkyl-2-phenyl-thiomorpholine Ⅲ and some of its derivatives are structurally related to p-chlorophenylethylamine and chloropromzine since they may be regarded as the open ring analogs of chloropromazine and bear the phenylethylamine structure as well. They were synthesized in five steps starting from the corresponding α-bromophenylacetic acid ethyl esters. Among them Ⅲ_d showed protective activities against ionization radiation in mice.更多还原