20,23-DIDEOXY-23-ALKYLENEIMINO-20-SUBSTITUTED AMINOMYCAMINOSYL RELONOLIDE

摘要

NEW MATERIAL:The compound of formula I [n is 5 or 6: R1 is H or (hydroxy) lower alkyl; R2 is H, (hydroxy) lower alkyl, or aralkyl; R3 is H or OH; R1 and R2 may together with N atom bonded thereto form 5-13-membered alkyleneimino, or the group NR1(R2) may be azido group]. EXAMPLE:20, 23-Dideoxy-20-N-methylbenzylamino-23-hexamethyleneiminomycaminosyl relonolide. USE:An antibacterial agent effective to Gram-positive and Gram-negative bacteria. PREPARATION:20,23-Dideoxy-20-halo-23-alkyleneimino mycaminosyl relonolide of formula II (X is halogen) is made to react with the amine of formula III usually in an aprotic solvent such as THF, acetonitrile, etc., preferably under heat refluxing.