PRODUCTION OF 16-MEMBERED CYCLIC MACROLIDE BASED COMPOUND

摘要

PURPOSE:To obtain the titled compound as an antimicrobial agent in high yield, by reacting a tin-containing 16-membered cyclic macrolide based compound having an specific dissacharide residue with a specific halide to effect selective acylation and alkylation of OH-group at the 4''-position without protecting OH-group at the 4'''-position. CONSTITUTION:A tin-containing 16-membered cyclic macrolide based compound having a dissacharide residue expressed by formula I (R<1> represents H or OH protected with a readily eliminate protecting group) is reacted with a halide expressed by the formula R<2>X [R<2> represents (substituted) alkyl or acyl; X represents halogen atom] to obtain the aimed compound having the dissacharide residue expressed by formula II at the 5-position. A compound expressed by formula III (either one of R<3> and R<4> represents H, and the other represents H, D-forosamino, etc.; R<5> represents H or methyl; R<6> and R<7> together link to represent single bond, etc.; R<8> represents H, methyl, etc.; R<9> represents methyl, etc.; R<10> represents OH, etc.; R<11> represents methyl, etc.) is a novel substance.