The described synthetic route to Orforglipron demonstrates a practical, scalable, and high-yielding approach to a structurally complex oral GLP-1 receptor agonist.
What are GLP-1 receptor agonists? Shortly after food intake, the human body releases a hormone called glucagon-like peptide-1. That hormone binds to receptors on certain cells, triggering the body to suppress glucagon, release insulin, and slow digestion. These combined metabolic effects generate that familiar feeling of fullness after a ...
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 ...
ChemAIRS optimized Eli Lilly's oral GLP-1 agonist Orforglipronstreamlining synthesis of key intermediates and scale-up conditions for commercial production. Accelerate your metabolic drug development with AI-driven retrosynthesis solutions.
The increasing prevalence of type 2 diabetes presents a major global health challenge. Glucagon-like peptide-1 (GLP-1) receptor agonists offer glycemic control, weight loss, and cardiovascular benefits but are limited by rapid enzymatic degradation and short half-life. Semaglutide, modified with a C18 diacid, extends its half-life to one week.
In this study, a series of fused-heterocyclic derivatives were systematically designed and synthesized using an efficient route, and evaluated in terms of GLP-1R agonist activity. We employed short synthetic steps and reactions that are tolerant of ...
