Novel synthesis of Abaloparatide: Advancing osteoporosis treatment in postmenopausal women

[Display omitted] •Soluble hydrophobic support-assisted liquid-phase synthesis technology of Abaloparatide.•Conditions of removing support Tag-OH.•Improving the synthesis conditions of Fragment 4. Abaloparatide, a novel parathyroid hormone-related peptide, emerges as a leading drug for treating oste...

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Veröffentlicht in:Tetrahedron letters 2024-09, Vol.147, p.155228, Article 155228
Hauptverfasser: Zhang, Na, Zhang, Huazheng, Teng, Yuetai, Yin, Xiaoxue, Niu, Weihong, Qin, Yinhui, Xu, Nan
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Sprache:eng
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Zusammenfassung:[Display omitted] •Soluble hydrophobic support-assisted liquid-phase synthesis technology of Abaloparatide.•Conditions of removing support Tag-OH.•Improving the synthesis conditions of Fragment 4. Abaloparatide, a novel parathyroid hormone-related peptide, emerges as a leading drug for treating osteoporosis in postmenopausal women at high risk of fracture. The therapeutic agent has demonstrated efficacy in significantly enhancing bone mineral density, fortifying bone strength, and stimulating bone formation. Developing a synthetic route for Abaloparatide with high-yield and purity products is of paramount importance. This paper reported a newly developed liquid-phase synthetic method based on soluble hydrophobic support assistance for the total synthesis of Abaloparatide, which has proven to be simple, scalable, and highly effective. The optimization of reaction conditions has yielded Abaloparatide with both high yield and purity, producing satisfactory results.
ISSN:0040-4039
DOI:10.1016/j.tetlet.2024.155228