氘标记天018的制备

Deuteration of α-sec-Butyl-p-Hydroxybenzyl Alcohol

以自制天018为原料,经碘化后,甲醇为溶剂,钯/碳为催化剂,于氘气环境中非均相催化氘化还原脱碘,获得了质谱分子离子峰峰高比为2.3:1的二氘代、一氘代天018的混合标记物,该产品已提供给临床研究。

It has been proved that α-sec-butyl-p-hydroxybenzyl alcohol (T-018) is a strong sedative and an ticonvulsant. Deuterated T-018 was prepared as a tracer for studying the metabolism of T-018. 2-Iodo-T-018 (2. 10 g), prepared by the iodination of T-018 using chloramine T, was dissolved in 70 ml methanol and,after the addition of 750 mg 5% Pd/C and 15 ml triethylamine,treated with deuterium gas for 9 h. A mixture of mono-and di-deuterated T-018 was obtained;yield was 84.77 %. Molecular clustering as determined ...