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<p>In previous studies, we discovered YZD-7082B, a selective estrogen receptor degrader (SERD) with excellent comprehensive properties. Here, we reported the development of an efficient multigram-scale synthetic process for YZD-7082 in 13 steps. The route featured a chiral resolution of a thiochroman intermediate with a unique <i>cis</i>-1,2-diaryl motif using a chiral amine and a mild reduction of amide using ZnEt<sub>2</sub>/LiCl/(EtO)<sub>3</sub>SiH system. This approach also overcomes the issues of high loadings of palladium catalysts and long reaction time. The developed process provided YZD-7082B with an HPLC purity of &gt; 99.8% and ee of &gt; 99%.</p> Graphical Abstract <p></p>

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A practical synthesis of YZD-7082B, a novel orally bioavailable selective estrogen receptor degrader (SERD) for the treatment of ER+ breast cancer

  • 期刊论文

  • 发表日期：

    2025年3月16日

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  • Yongqi He,
  • Xin-Yu Leng,
  • Runying Wang,
  • Lulu Sun,
  • Dan Zhang,
  • Yushe Yang

摘要

In previous studies, we discovered YZD-7082B, a selective estrogen receptor degrader (SERD) with excellent comprehensive properties. Here, we reported the development of an efficient multigram-scale synthetic process for YZD-7082 in 13 steps. The route featured a chiral resolution of a thiochroman intermediate with a unique cis-1,2-diaryl motif using a chiral amine and a mild reduction of amide using ZnEt2/LiCl/(EtO)3SiH system. This approach also overcomes the issues of high loadings of palladium catalysts and long reaction time. The developed process provided YZD-7082B with an HPLC purity of > 99.8% and ee of > 99%.

Graphical Abstract