Preparation method of isavuconazonium monosulfate through oxidation-reduction reactions

2017 
The invention discloses a preparation method of isavuconazonium monosulfate through oxidation-reduction reactions. According to the preparation method, isavuconazole, N-methyl-N-(3-[((N-t-butyloxycarboryl-N-methylamino)acetoxyl)methyl]pyridine-2-yl) (1-chloroethyl)carbamate, and iodine salts carry out reactions to obtain iodine salts of isavuconazonium with protected Boc; then the iodine salts of isavuconazonium with protected Boc is oxidized by CuSO4 to obtain sulfate of isavuconazonium with protected Boc; and finally the Boc is removed by sulfuric acid to obtain isavuconazonium monosulfate. The preparation method has the advantages that the ratio of salt forms of isavuconazonium monosulfate can be precisely controlled, the operation is simple, complicated steps such as trisulfate pH value adjustment, salt form converse through ion exchange, and the like are avoided, the total purity can reach more than 98&, and the indexes of related substances are qualified.
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