| abstract |
PURPOSE:To obtain the titled substance, by reducing the axido group in a 4(R) coordinated compound having the azide group into an amino group, acylating the amino group, substituting the substituent group at the 4-position or sulfonating the 1-position in any order. CONSTITUTION:A compound of formula I [R is halogen or OSO2R<1>(R<1> is methyl, ethyl, phenyl, p-methylophenyl, p-bromophenyl or benzyl)] is subjected to the following reactions; (A) reduction of the azido group into an amino group, (B) acylation of the amino group, (C) substitution reaction of the group R at the 4-position or (D) sulfonation of the nitrogen atom at the 1-position to give a compound of formula II(R<2> is acryl, R<3> is H, OH, azido, dithiocarbamate, nitro, cyano, etc.; M is H or cation). The reaction (A) is carried out by the catalytic reduction in the presence of Pd or Ni, etc. as a catalyst, and the reaction (B) is carried out by the conventional method for synthesizing peptides. The reaction (C) is carried out in the presence of a capturing agent for a halogen, etc., which is an eliminative group. USE:An antimicrobial active agent. |