Process Development and Crystallization in Oiling-Out System of a Novel Topical Antiandrogen

    January 2017 in “ Organic Process Research & Development ”
    Sebastien Daver, Nicolas Rodeville, Francois Pineau, Jean-Marie Arlabosse, Christine Moureou, Franck Muller, Romain Pierre, Karinne Bouquet, Laurence Dumais, Jean-Guy Boiteau, Isabelle Cardinaud
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    Studysummary This article describes the efficient synthesis of (S)-N-(2-bromo-6-methoxypyridin-4-yl)-2-hydroxy-2,4-dimethylpentanamide, a novel topical antiandrogen, with high purity and enantiomeric excess but reports no pharmacological results.
    Our plain-language summary. Not medical advice or a treatment recommendation. Consult a qualified healthcare professional before changing treatment. Full disclaimer
    In 2017, researchers developed an efficient method for producing a new topical antiandrogen, (S)-N-(2-bromo-6-methoxypyridin-4-yl)-2-hydroxy-2,4-dimethylpentanamide 1, on a kilogram scale with an overall yield of 25% and a purity of 98.8%. The process involved a key amide coupling, the use of a temporary protecting group, and a final crystallization step. The compound was designed for the treatment of excess sebum and acne. The document does not mention any study involving people or any subjects related to hair loss, alopecia, or hair growth.
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