TYROSIN DERIVATIVES AND PROCESS FOR PRODUCTING THE SAME

摘要

Tylosin derivatives represented by the following general formula (I): [wherein R denotes a hydrogen atom, acetyl, propionyl or a radical of Si(R<2>)3 (in which R<2> is a lower alkyl group), and R<1> stands for a hydrogen atom or a radical of Si(R<2>)3] are novel compounds, which are useful as intermediates for the synthesis of 4 sec -acyl derivatives of tylosin because, after introduction of any desired acyl group at the 4 sec -hydroxyl group, the silyl protective group can be readily removed without liberation of said acyl group. This invention also provides processes for producing said tylosin derivatives. More specifically, it provides a method of selectively protecting 2 min - and 4'''-hydroxyl groups of tylosin (those of higher reactivity among the hydroxyl groups involved); a method of selectively protecting only the 4'''-hydroxyl group of tylosin; a method of selectively protecting the 3- and 4'''-hydroxyl groups of 2 min -O-acyltylosin; and a method of protecting 3-, 2 min - and 4'''-hydroxyl groups of tylosin.