Glucagon-like peptide-1 receptor agonists are known and effective treatments for type 2 diabetes. Presently these therapies are available only as peptide formulations, mostly injectables. Many patients prefer an oral regimen and so there has been industry interest in an effective small molecule treatment due to the difficulties with oral peptide administration. LY3502970 has been identified as a potent and selective GLP-1R agonist but its development has included several challenges. The process leading to the final API target LY3502970 encompasses 28 chemical transformations to build and join three fragments. Each of the three fragments has been synthesized by multiple routes on production scale with each route improvement focusing on safety and environmental impact, yield and selectivity, and impurity profiles. The route selection and process definition programs for this complex and relatively high molecular weight small molecule will be described.

Process improvements for the highly convergent synthesis of a complex small molecule API

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