The Preparation and Synthesis of Buserelin
Author(s): DONG Qian, JU Ying-ying, XU Hong-wei, YE Xiao-hui, CHENG Mei-ling, KONG Yi, Nanjing Stomatological Hospital, School of Life Science & Technology, China Pharmaceutical University
Pages: 412-415
Year: 2014 Issue: 5
Journal: Pharmaceutical Biotechnology
Keyword: Buserelin; Solid phase synthesis; GnRH; Polypeptide;
Abstract: Buserelin is the peptide drug transformed based on gonadotropin-releasing hormone( GnRH). It is mainly used for the treatment of breast cancer,prostate cancer and other diseases in clinical. This paper mainly studies buserelin synthesis: The DIC /HOBT as the condensing agent,Boc and Fmoc associated synthetic method for synthesis of solid phase synthesis,using ethylamine /methanol solvent as cutting fluid which can release the C-terminal ethylamine-peptide from the resin directly. And synthetic products received structural identification. Purity of the final product was 97%. The synthetic method is simple,and by it a high purity of product is obtained,so it is suitable for buserelin process development.
Pages: 412-415
Year: 2014 Issue: 5
Journal: Pharmaceutical Biotechnology
Keyword: Buserelin; Solid phase synthesis; GnRH; Polypeptide;
Abstract: Buserelin is the peptide drug transformed based on gonadotropin-releasing hormone( GnRH). It is mainly used for the treatment of breast cancer,prostate cancer and other diseases in clinical. This paper mainly studies buserelin synthesis: The DIC /HOBT as the condensing agent,Boc and Fmoc associated synthetic method for synthesis of solid phase synthesis,using ethylamine /methanol solvent as cutting fluid which can release the C-terminal ethylamine-peptide from the resin directly. And synthetic products received structural identification. Purity of the final product was 97%. The synthetic method is simple,and by it a high purity of product is obtained,so it is suitable for buserelin process development.
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