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The synthesis of 2,6-dichlorobenzylidene aminoguanidine acetate [α-14C]
Journal of Labelled Compounds and Radiopharmaceuticals ( IF 0.9 ) Pub Date : 1976-10-01 , DOI: 10.1002/jlcr.2580120404
Samuel F. Sisenwine , Cesario O. Tio , Jenny Ahern

2,6-Dichlorobenzylidene aminoguanidine acetate, a new antihypertensive agent, was labelled with 14C at the benzal position for metabolic studies. The key reaction involved the reduction of the sterically hindered 2,6-dichlorobenzonitrile [cyano-14C] with lithium aluminum hydride to 2,6-dichlorobenzaldehyde [carbonyl-14C]. The labelled nitrile was prepared by a Sandmeyer reaction employing 2,6-dichloroaniline and K14CN. Further reaction of the labelled aldehyde with aminoguanidine bicarbonate produced the desired radioactive drug.

中文翻译:

2,6-二氯亚苄基氨基胍乙酸酯[α-14C]的合成

2,6-二氯亚苄基氨基胍醋酸盐是一种新型抗高血压药,在苯甲位用 14C 标记用于代谢研究。关键反应涉及用氢化铝锂将空间位阻的 2,6-二氯苯甲腈 [氰基-14C] 还原为 2,6-二氯苯甲醛 [羰基-14C]。标记的腈通过使用 2,6-二氯苯胺和 K14CN 的 Sandmeyer 反应制备。标记的醛与氨基胍碳酸氢盐的进一步反应产生所需的放射性药物。
更新日期:1976-10-01
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