A practical kilogram scale chromatography-free synthesis of stearoyl-CoA desaturase 1 (SCD1) inhibitor MK-8245 is described. The key features of this sequence include an efficient addition–elimination reaction of a piperidine fragment with a 3-bromoisoxaline followed by an iodine-mediated oxidation to the corresponding isoxazole. The development of a safe and scalable tetrazole formation protocol is also presented.

中文翻译：

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开发实用合成硬脂酰辅酶A去饱和酶（SCD1）抑制剂MK-8245

描述了一种实用的无千克规模层析的硬脂酰-CoA去饱和酶1（SCD1）抑制剂MK-8245合成方法。该序列的关键特征包括：哌啶片段与3-溴异己啉的有效加成-消除反应，然后由碘介导氧化为相应的异恶唑。还介绍了安全和可扩展的四唑形成方案的开发。