Kilogram-Scale Synthesis of Osteogenic Growth Peptide (10鈥?4) Using a Fragment Coupling Approach
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- 作者：Teng Zhang ; Zhenxing Chen ; Yan Tian ; Bin Han ; Ning Zhang ; Wei Song ; Zhulan Liu ; Jinli Zhao ; Jianli Liu
- 刊名：Organic Process Research & Development
- 出版年：2015
- 出版时间：September 18, 2015
- 年：2015
- 卷：19
- 期：9
- 页码：1257-1262
- 全文大小：299K
- ISSN：1520-586X
文摘
Kilogram-scale synthesis of a bioactive pentapeptide in solution by 鈥? + 2鈥?fragment coupling strategy has been successively accomplished in the development of OGP (10鈥?4), a minimal OGP-derived sequence that retains the full proliferative activity of the osteogenic growth peptide. The synthetic scheme, coupling conditions, and scaling-up of the process are systematically studied; the epimerization of the tripeptide fragment and pentapeptide are also evaluated.