Norgestomet is a synthetic progesterone derivative applied in veterinary medicine to control estrus and ovulation in cattle. Norgestomet has been widely used in the livestock industry to promote the synchronization of estrus in cattle and increase pregnancy rates. However, highly reproducible synthetic methods for Norgestomet have been rarely reported. Here, we described a method for the synthesis of Norgestomet and performed quantitative NMR analysis to determine the purity of the products. Moreover, the agonistic activity of the synthesized compounds against progesterone receptors (PRs) was evaluated using an alkaline phosphatase assay. We synthesized Norgestomet with 97.9% purity that exhibited agonistic activity against PR with EC₅₀ values of 4.5 nM. We also synthesized the 17β-isomer of Norgestomet with 92.7% purity that did not exhibit any PR agonistic activity. The proposed synthetic route of Norgestomet can facilitate the assessment of residual Norgestomet in foods.

Norgestomet 是一种合成黄体酮衍生物，用于兽医控制牛的发情和排卵。Norgestomet已广泛用于畜牧业，以促进牛发情同步并提高妊娠率。然而，很少报道用于 Norgestomet 的高度可重复的合成方法。在这里，我们描述了一种合成 Norgestomet 的方法，并进行了定量 NMR 分析以确定产品的纯度。此外，使用碱性磷酸酶测定法评估了合成化合物对孕酮受体 (PRs) 的激动活性。我们合成了纯度为 97.9% 的 Norgestomet，其对 PR 具有激动活性，EC ₅₀值为 4.5 nM。我们还合成了纯度为 92.7% 的 Norgestomet 的 17β-异构体，没有表现出任何 PR 激动活性。所提出的 Norgestomet 合成路线有助于评估食品中残留的 Norgestomet。