~(14)C-标记1,2-双-(3,5-二氧哌嗪基)乙烷ICRF_(154)的合成

SYNTHESIS OF ~(14)C-LABELLED 1, 2-BIS(3,5-DIOXO PIPERAZIN-1-YL)ETHANE(ICRF_(154))

  • 摘要: <正> A.M.Greighton 1969年合成了双酰胺环ICRF_(154),然后改变化学结构合成了ICRF_(159,193)等衍生物。对其抗肿瘤(肉瘤S_(180)),白血病L_(1210),腺癌175,肿瘤walker_(256)进行药物筛选。ICRF_(154)口服对实验肿瘤有效,Dr.Hellmann临床试用发现不活泼。由于它在水和有机溶剂中不溶解,认为体内吸收很差或不吸收。我所将ICRFF_(154)用于临床治疗银宵病疗效显著。~(14)C-标记ICRF_(154)可为进行吸收、分布、排泄研究提供标记化合物。

     

    Abstract: The antitumour compound ICRF 154 was orally effective against a number ofexperimental tumours. It showed neither activity nor toxicity in a preliminaryclinical trial. We also found it useful in the treatment of psoriasis ~(14)C-labelled ICRF 154 was synthesized (for absorption, distribution andexcretion studies) in three steps, using (carboxy-~(14)C) carboxylic acid as thelabelled starting material. The radiochemical purity was 99.8%, as determinated by thin-laryer radio-chromatography; and specific activity, 3 Ci/mol. Radiochemical yield was 30%.

     

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