Erythromycin derivative and process for preparing the same

Claim 1

A compound, or a salt thereof, represented by the general formula: wherein R 1 stands for a hydrogen atom or an acyl radical which may be substituted; R 2 stands for a hydrogen atom, an acyl or alkyl radical which may be substituted; R 3 stands for a hydrogen atom or a methyl radical; R 4 stands for a hydrogen atom or a hydroxy radical; Z stands for the formula (wherein R 5 stands for a hydrogen atom, an acyl or alkyl radical which may be substituted, and R° stands for a hydrogen atom, an acyl radical of a lower carboxylic acid or an alkyl radical which may be substituted by an alkylthio radical), the formula (wherein R 7 stands for a hydrogen atom, an acyl or alkyl radical which may be substituted), the formula [wherein Y stands for the formula B-R (wherein R 8 stands for an alkyl or aryl radical), or the formula wherein each of R 9 and R 10 , which may be the same or different, stands for a hydrogen atom or an alkyl radical, or constitutes a cyclic alkyl radical with the adjacent carbon atom, or either of R 9 and R 10 is a hydrogen atom, an alkyl radical or an arvl radical while the other is a dialkylamino radical)]; R a stands for the formula (wherein R b stands for a hydrogen atom, a lower alkyl or cycloalkyl radical, R c stands for a hydrogen atom, a lower alkyl, cycloalkyl, lower alkenyl or lower alkynyl radical which may be substituted, or R b and R c form a cyclic alkylamino radical together with the adjacent nitrogen atom), or the formula (wherein R d stands for a lower alkyl radical, each of R e and R f , which may be the same or different, stands for a lower aklyl, cycloalkyl, lower alkenyl or lower alkynyl radical which may be substituted, or R e and R f form a cyclic alkylamino radical together with the adjacent nitrogen atom, and X stands for an anion); and stands for the formula (wherein R 11 and R 1 2 both stand for hydrogen atoms or both taken together form a chemical bond), when R a is the formula or stands for the formula (wherein R 11 and R 12 have the same meanings as defined above) or the formula (wherein R ° stands for a hydrogen atom or lower alkyl), when R a is the formula with proviso that each of R 1 , R 2 , R 4 , R 5 and R 6 is not a hydrogen atom at the same time, when R a is a dimethylamino radical and R 3 is a methyl radical; each of R 1 , R 2 , R 4 and R 7 is not a hydrogen atom at the same time, when R a is a dimethylamino radical and R 3 is a methyl radical; R 5 is neither a hydrogen atom nor a mesyl radical and R 6 is not a hydrogen atom at the same time or Y is not =O, when R a is a dimethlamino radical, R 11 and R 12 taken together form a chemical bond, R l , R 2 and R 4 are each hydrogen atoms and R 3 is a methyl radical; R 5 is neither a hydrogen atom nor a mesyl radical and R 6 is not a hydrogen atom, when R a is a dimethlamino radical, R 11 and R 12 taken together form a chemical bond, R 1 is an acetyl radical, R 2 is a formyl radical, R 3 is a methyl radical and R 4 is a hydrogen atom; each of R 2 , R 5 and R 6 is not a hydrogen atom at the same time, when R a is a dimethylamino radical, R 11 and R 12 taken together form a chemical bond, R 1 is an acetyl, propionyl or 3-ethoxycarbonylpropionyl radical, R 3 is a methyl radical and R 4 is a hydrogen atom; Y is not when R a is a trimethylammonio radical, R 11 and R 12 taken together form a chemical bond, each of R 1 , R 2 and R 4 is a hydrogen atom and R 3 is a methyl radical; each of R 1 , R 2 , R 4 , R 5 and R 6 is not a hydrogen atom at the same time, each of R 1 , R 2 , R 4 , and R 7 is not a hydrogen atom at the same time, or R 1 is neither a propionyl nor an ethoxycarbonyl radical and each of R 2 , R 4 , R and R 6 is not a hydrogen atom, when R a is a trimetylammonio radical, is the formula and R 3 is a methyl radical; and is not the formula and R 1 is not an acyl radical, when either R e or R f is an alkyl radical substituted by a 1-acyloxy radical.