Method for increasing yield of amikacin

• Main Authors: CHU JIE, ZHANG ZHAOZHEN, CAI CHENGWEI, WU KE, GU ZONGSHUAI, SUN ZHENGJUN, WANG SHICHUAN, LI BAOYONG, FAN CHANGYING, DONG TINGHUA
• Format: Patent
• Language: English
• Published: 18.02.2015
• Subjects: CHEMISTRY; CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION ORPROCESSING OF GOODS; DERIVATIVES THEREOF; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; METALLURGY; NUCLEIC ACIDS; NUCLEOSIDES; NUCLEOTIDES; ORGANIC CHEMISTRY; SUGARS; 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 method for increasing yield of amikacin. The method for increasing yield of amikacin comprises the following steps: heating, refluxing and carrying out reaction on gamma-amino-alpha-hydroxybutyric acid and fluorenylmethyl chloroformate, so as to generate a reaction liquid containing gamma-amino-alpha-hydroxybutyric acid; directly adding N-hydroxyl phthalimide and N,N-dicyclohexylcarbodiimide into the reaction liquid, and carrying out reaction to generate a reaction liquid containing active ester; directly adding a kanamycin A silanization compound into the reaction liquid containing the active ester for carrying out acylation reaction, after complete reaction is finished, adding an HBr aqueous solution until the pH is adjusted to be 2-3, and carrying out suction filtration to remove solid impurities; and then carrying out reduced pressure distillation for removing the solvent, adjusting the pH to be 7-8 with concentrated liquor, purifying by virtue of a CD180 macroporous resin column, concentrating, and carrying out freeze drying, so that amikacin solid is obtained. The active ester causes selectivity of the acylation reaction to be greatly improved due to enlargement of a protective group, and a follow-up processing step is also greatly simplified, so that the amikacin synthesis yield is increased.