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Synthesis of [3 H] and [14 C]Genipin
Journal of Labelled Compounds and Radiopharmaceuticals ( IF 0.9 ) Pub Date : 2020-02-11 , DOI: 10.1002/jlcr.3832 Adele E Queen 1 , David Hesk 2 , David M Lindsay 1 , William J Kerr 1 , Kenneth Rehder 2 , Tim Fennell 2 , Wayne Mascarella 2 , Desong Zhong 2 , Scott Runyon 2
Journal of Labelled Compounds and Radiopharmaceuticals ( IF 0.9 ) Pub Date : 2020-02-11 , DOI: 10.1002/jlcr.3832 Adele E Queen 1 , David Hesk 2 , David M Lindsay 1 , William J Kerr 1 , Kenneth Rehder 2 , Tim Fennell 2 , Wayne Mascarella 2 , Desong Zhong 2 , Scott Runyon 2
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[3 H]Genipin was synthesized in a single step by Ir(I) catalyzed hydrogen isotope exchange. Conditions for selective exchange of the sp2 CH bond ortho to the methyl ester functionality were developed through deuterium modeling studies through a catalyst screen. Optimized conditions so obtained were then utilized with tritium gas to generate [3 H]genipin at a specific activity of 18.5 Ci/mmol. Racemic [14 C]genipin was prepared in 8 steps in overall 5.4% radiochemical yield from potassium [14 C]cyanide.
中文翻译：
[3 H]和[14 C]京尼平的合成
[3 H]京尼平是通过 Ir(I) 催化氢同位素交换一步合成的。通过催化剂筛选进行氘建模研究，开发了与甲酯官能团邻位的 sp2 CH 键选择性交换的条件。然后将如此获得的优化条件与氚气一起使用以产生比活度为18.5 Ci/mmol的[3H]京尼平。由[14C]氰化钾分8步制备外消旋[14C]京尼平，总放射化学产率为5.4%。
更新日期：2020-02-11
中文翻译：
[3 H]和[14 C]京尼平的合成
[3 H]京尼平是通过 Ir(I) 催化氢同位素交换一步合成的。通过催化剂筛选进行氘建模研究，开发了与甲酯官能团邻位的 sp2 CH 键选择性交换的条件。然后将如此获得的优化条件与氚气一起使用以产生比活度为18.5 Ci/mmol的[3H]京尼平。由[14C]氰化钾分8步制备外消旋[14C]京尼平，总放射化学产率为5.4%。
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