An improved synthesis of SGD-11275 was developed to address inefficiencies in cost, time, and safety associated with the previous supply route. The new route features a Buchwald-Hartwig amination with acetamide optimized by high-throughput experimentation as well as a GaCl₃-mediated Friedel–Crafts acylation. Subsequent amide hydrolysis was demonstrated from the isolated Friedel–Crafts product and as a through-process with equal effectiveness. The new route reduced the commercial synthesis by three steps and increased the overall yield by 18.6%.

中文翻译：

---

利用 Pd 催化的乙酰胺芳基化反应和镓介导的 Friedel-Crafts 酰化反应合成 SGD-11275 的工艺开发


开发了 SGD-11275 的改进合成，以解决与以前的供应路线相关的成本、时间和安全性低效率问题。新路线的特点是通过高通量实验优化的含乙酰胺的 Buchwald-Hartwig 胺化反应，以及 GaCl₃ 介导的 Friedel-Crafts 酰化反应。随后的酰胺水解从分离的 Friedel-Crafts 产品中得到证明，并且作为一个贯穿过程具有相同的有效性。新路线将商业合成减少了三个步骤，并将总产量提高了 18.6%。