Development of a Modified Process for the Kilogram-Scale Synthesis of c-Met/ALK Inhibitor HS-10168

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• 作者：Jun YuJinJia Wang
• 刊名：Organic Process Research & Development
• 出版年：2017
• 出版时间：January 20, 2017
• 年：2017
• 卷：21
• 期：1
• 页码：133-137
• 全文大小：276K
• ISSN：1520-586X

文摘

A modified synthetic route to c-Met/ALK inhibitor HS-10168 has been developed on a kilogram scale. The key steps of the new process include a Suzuki coupling reaction of nitro-containing bromopyridine 6 and para-phenol boronate 9 to give intermediate 10, which was then converted to its triflate 11. The phosphorus group was introduced by coupling of 11 and dimethylphoshine oxide 8 to give compound 12, which was reduced to produce HS-10168.