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Kilogram-Scale Synthesis of 11β-Hydroxyandrosterone

 

In this paper, the authors describe a robust and large-scale synthesis of the ketosteroid building block 11β-hydroxyandrosterone from cheap and readily available starting materials. The initial discovery route was redesigned incorporating two stereoselective steps and optimized to minimize chromatographic purification. The process route was then conducted on kilogram scale delivering a significantly enhanced yield over fewer steps.


Hossay Abas, Peter Blencowe, Ellen MacDonald, Emma Stanway, Eric P. A. Talbot, Haiyang Wang, Morag Watson, Jin Zhang, and Lucy A. Harwood
Organic Process Research & Development 2024 28(7), 2692-2701
DOI: 10.1021/acs.oprd.4c00084

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