ArticleMolecules (Basel, Switzerland)2025
Development of a Multigram Synthetic Route to RM-581, an Orally Active Aminosteroid Derivative Against Several Types of Cancers.
Article in Molecules (Basel, Switzerland), 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.
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1 citing paper in PubMed.
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4 authors.
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Abstract
Aminosteroid derivative RM-581 stands out as an anticancer agent, supported by positive in vitro and in vivo studies on resistant cancers of the breast, prostate, and pancreas. A synthetic route has already been developed to obtain aminosteroid RM-581 in small quantities (scale of milligrams to a few grams). However, this route has significant limitations in view of its transposition to scaling up to larger quantities to support late preclinical and clinical trials. Among the problems are the use of toxic reagents, the moderate overall yield, and the need for multiple purifications through chromatographic columns. The development of a new synthetic route has therefore been explored. Starting from commercially available estrone, 2,4-dibromo-estrone was rapidly formed, followed by the regioselective introduction of a nitro group at the C2 position and by the methylation of phenol at the C3 position. The 4-bromo-2-nitro-3-
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