METHOD OF PREPARING DERIVATIVES OF 6-N-METHYLKANAMYCING A AND B

摘要

Semisynthetic derivatives of kanamycin A and B of the formula IV in which R3 and R have the meaning stated in Claim 1 are prepared. The process starts from corresponding compounds with R = hydrogen and comprises acylation with an acylating agent of the formula VII in which W and M have the meaning stated in Claim 1, and subsequent elimination of the amino protective group W. A preferred acylating agent of the formula VIIa is obtained in situ by mixing the appropriate N-protected carboxylic acid with equimolar amounts of N-hydroxy-5-norbornene-2,3-dicarboximide and dicyclohexylcarbodiimide as dehydrating agent. The said compounds have antibacterial activity and can therefore be used in medicines or as additives to animal feedstuffs.