Bivalirudin solid-phase synthesis method

• Main Authors: LI YINGXIN, ZHANG QI, YAO ZEYU, LENG GUOQING, WANG LILI, YANG WENLONG, TIAN HUI, SHEN QINGBO
• Format: Patent
• Language: English
• Published: 22.04.2015
• Subjects: CHEMISTRY; CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION ORPROCESSING OF GOODS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; METALLURGY; ORGANIC CHEMISTRY; PEPTIDES; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS; TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINSTCLIMATE CHANGE

The invention discloses a bivalirudin solid-phase synthesis method. The method comprises the steps of synthetizing Fmoc-Leu-carrier resin with Wang resin as the starting material, and sequentially connecting corresponding Fmoc-protected amino acid in the following sequence to the Fmoc-Leu-Wang resin with the solid-phase coupling synthetizing method to obtain bivalirudin resin, wherein during X fragment connection, solid-phase coupling synthetizing reaction is conducted, and the Fmoc-protected amino acid corresponding to the X fragment is Fmoc-Gly-Gly-OH. By the adoption of the method, generation of technological impurities bivalirudin [-Gly] and bivalirudin [+Gly] is avoided, purifying difficulty is reduced greatly, and yield is increased.