The target compound PF-06878031 is a key structural fragment of a range of oral late-stage glucagon-like peptide-1 receptor agonists (GLP-1-RA) under development in our laboratories for the indications of type-2 diabetes mellitus (T2DM) and weight loss. This article describes the identification of a selective alkylation route and development of a process, capable of delivering multikilo quantities of PF-06878031. Process development afforded improved safety, increased yield, reduced step count, and lowered PMI. The new process has been scaled up at multiple facilities to generate >1.5MT of high purity PF-06878031.

中文翻译：

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PF-06878031 合成路线的开发第 1 部分：选择性烷基化路线

目标化合物PF-06878031是我们实验室正在开发的一系列口服晚期胰高血糖素样肽-1 受体激动剂 (GLP-1-RA) 的关键结构片段，用于治疗 2 型糖尿病 (T2DM) ）和减肥。本文介绍了选择性烷基化路线的识别和工艺的开发，能够提供数千份PF-06878031。工艺开发提高了安全性、提高了产量、减少了步骤数并降低了 PMI。新工艺已在多个工厂进行规模化生产，可生成 >1.5MT 的高纯度PF-06878031。