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Pd-Catalyzed Arylation in the Synthesis of a GABA r2/3 Agonist

有机合成与工艺文献分享 2025-03-28 08:51
文章摘要
本文报道了一种替代合成GABA α2/3-agonist候选药物62的方法，以支持临床试验。与初始合成59类似，由于所需的硼酸昂贵且产生废物，Suzuki–Miyaura偶联必须被替换。作者开发了一种多克规模的C-H活化方法，通过将类似的杂环60与芳基氯61偶联。作者提出，通过使用Bu4NHSO4作为添加剂，可以稳定阴离子Pd0物种，从而实现催化剂周转。反应优化表明，通过使用1,4-二氧六环作为溶剂在90°C下可以避免Dimroth重排产生的2-芳基化产物和双芳基副产物。芳基氯61替代了硼酸偶联伙伴，降低了成本并提高了方法的原子经济性。经过重结晶，C-H芳基化产物62的收率为87%。
Pd-Catalyzed Arylation in the Synthesis of a GABA r2/3 Agonist
查看文献： The Expedient Synthesis of 4,2‘-Difluoro-5‘-(7-trifluoromethyl- imidazo[1,2-a]pyrimidin-3-yl)biphenyl-2-carbonitrile, a GABA α2/3 Agonist
查看期刊：Organic Process Research & Development
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