Practical and Efficient Synthesis of 2-Thio-imidazole Derivative-ZY12201: A Potent TGR5 Agonist
ORGANIC PROCESS RESEARCH & DEVELOPMENT(2020)
摘要
Early scalable process development for the synthesis of ZY12201, a novel TGR5 receptor agonist, as a potential clinical candidate is described. A practical, efficient, and scalable synthetic route provided ZY12201 in seven steps and 32% overall yield. The key step involves an inexpensive acetic acid-mediated cyclization of thiourea 6 for the construction of 2-thio-imidazole derivative 7. The developed process demonstrated cost-effective, high-yielding, kilogram-scalable, and environmentally friendly synthesis of ZY12201. This high-yielding route enabled us to rapidly synthesize large quantities of ZY12201 in 99% purity to support in vivo and toxicity studies.
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关键词
TGR5,TGR5 agonist,type 2 diabetes,2-thio imidazole,1,2-dibromo ethane
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