Preparation method of 1-N-ethyl gentamicin C1a sulfate

• Main Authors: FENG CHENGJUN, LI XINGGANG, SU XIAOCHUN, BI XIAOMING, DI SHAOYAN, HU DONGHUI
• Format: Patent
• Language: Chinese; English
• Published: 29.12.2010
• Subjects: CHEMISTRY; DERIVATIVES THEREOF; METALLURGY; NUCLEIC ACIDS; NUCLEOSIDES; NUCLEOTIDES; ORGANIC CHEMISTRY; SUGARS

The invention discloses a preparation method of 1-N-ethyl gentamicin C1a sulfate. The method comprises the following steps of: carrying out a complexation reaction on gentamicin C1a and zinc acetate in a methanol solvent; then, dropping a mixed solution of acetic anhydride, triethylamine and tetrahydrofuran to carry out an acylation reaction and obtaining 3,2',6'-3-N-acetyl-gentamicin C1a by post-treatment; then, carrying out a silylation reaction with hexamethyl disilazane in a chloroform solvent; carrying out an N-alkylation reaction with acetaldehyde in a carrene solvent; then, carrying out a reduction reaction with potassium borohydride; hydrolyzing with an NaOH solution; obtaining 1-N-ethyl gentamicin C1a by post-treatment; adding the 1-N-ethyl gentamicin C1a to anhydrous ethanol or anhydrous methanol for stirring or dissolving; then, dropping concentrated sulfuric acid; and obtaining 1-N-ethyl gentamicin C1a sulfate by post-treatment. The method of the invention has higher yield.