Eptifibatide preparation method

US9394341B2 · kind B2 · utility

Assignee

• Chengdu Shengnuo BioTec Co., Ltd. · CN

Inventors

• Yongjun Wen · Lo Wu, CN
• Chuanbin Zhu · Chengdu, CN
• Xiaoli Wang · Mississauga, CA
• Yu-rim Han · Beijing, CN
• Guangbin Tong · Chengdu, CN

Key dates

• Filing date: Aug 9, 2012
• Grant date: Jul 19, 2016
• Expiry date: Aug 9, 2032

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07K14/75
• WIPO field: Biotechnology
• WIPO sector: Chemistry

Abstract

An Eptifibatide preparation method with product purity of more than 99.5%, the method comprising: using a solid phase polypeptide synthesis method to prepare eptifibatide resin, conducting acidolysis on the Eptifibatide resin to obtain a crude Eptifibatide linear peptide product, oxidizing to obtain a crude Eptifibatide product, purifying and exchanging salt to obtain an Eptifibatide finished product; the method using the solid phase polypeptide synthesis method to prepare the eptifibatide resin is: using a solid phase coupling synthesis method to sequentially splice a corresponding protective amino acid or a segment in the following sequence onto amino resin, and obtaining the Eptifibatide resin: X—Y-Trp(R1)-Pro-Cys(R2)-amino resin, wherein R1 is Boc or H, R2 is Trt or Acm, X is Mpr(R2)-Harg(R3), R3 is Pbf or H, and Y is Gly-Asp(OtBu).