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本文报导36个碳链上杂有醚键、硫醚键、胺键的双酰肼类化合物的合成.其合成法系由氧杂、硫杂、氮杂的二元酸二乙酯或4-苯基-1-哌嗪乙酸乙酯与水合肼缩合,生成相应酰肼,后者先与带有不同取代烃基的醛或酮缩合,再用钾硼氢还原制成;肼上带有苄基及苯乙基取代的酰肼系由相应酯与苄肼或苯乙肼直接缩合制得.经体内及体外单胺氧化酶抑制试验后找出了一个毒性很低,治疗指数较高的药物4-硫杂庚二酰(2-异丙基)肼(简称硫双肼),已推荐临床试用。
This paper reports the synthesis of 36 diacylhydrazines with ether linkage, thioether linkage and amine linkage on the carbon chain.The synthesis method consists of diacid, thia, aza and di The condensation of phenyl-1-piperazineacetate with hydrazine hydrate gives the corresponding hydrazide, which is first condensed with an aldehyde or ketone with a different substituted hydrocarbon group and then with potassium borohydride reduction; the hydrazine has a benzyl group And phenethyl substituted hydrazide from the corresponding ester and benzylhydrazine or phenelzine direct condensation obtained by in vivo and in vitro monoamine oxidase inhibition test found a very low toxicity, high therapeutic index of 4-thia Pimeloyl (2-isopropyl) hydrazine (thiadiazine for short) has been recommended for clinical trials.