The synthesis of one H-2 labeled and two H-3 labeled leukotriene C4 synthase inhibitors,Journal of Labelled Compounds and Radiopharmaceuticals

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The synthesis of one H-2 labeled and two H-3 labeled leukotriene C4 synthase inhibitors
Journal of Labelled Compounds and Radiopharmaceuticals ( IF 0.9 ) Pub Date : 2020-07-07 , DOI: 10.1002/jlcr.3862
Jonas Bergare ₁ , Lee Kingston ₁ , Dominic J Guly ₂ , James Dolan ₂ , Richard J Lewis ₃ , Charles S Elmore ₁

Affiliation

As part of a medicinal chemistry program aimed at developing a leukotriene C4 synthase inhibitor for the treatment of asthma, two tritium labeled and one stable isotope labeled compounds were required. The synthesis of the tritium labeled compounds used a standard bromination-tritiodehalogentation approach. One of the tritium labeled compounds was observed to exchange its tritium label slowly with the solvent. The stable isotope labeled compound was prepared in seven steps (3% overall yield) from [2 H6 ]acetone in a modification of the route used by medicinal chemistry.

中文翻译：

一种H-2标记和两种H-3标记白三烯C4合酶抑制剂的合成

作为旨在开发用于治疗哮喘的白三烯 C4 合酶抑制剂的药物化学计划的一部分，需要两种氚标记的化合物和一种稳定同位素标记的化合物。氚标记化合物的合成使用标准的溴化-氚硫脱卤化方法。观察到一种氚标记化合物缓慢地与溶剂交换其氚标记。稳定同位素标记的化合物是通过对药物化学路线的改进，由 [2 H6 ]丙酮分七步制备而成（总收率 3%）。

更新日期：2020-07-07

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