PURPOSE: To provide the subject new compound of specific structure, giving excellent enterokinesis-promoting activity, hardly degradable by gastric acid, thus capable of oral administration, few in side effects, thus useful for e.g. the treatment of digestive organ symptoms.
CONSTITUTION: N,2'-o-bis(benzyloxycarbonyl)-de(N-methyl)erythromycin A is dissolved in acetic acid followed by treatment to carry out hemiketalization, and the product is made to react with carbobenzoxychloride in the presence of a base and further with benzyl bromide in the presence of sodium hydride and then with methyl iodide in the presence of sodium hydride, and the reactional product is put to catalytic reduction in the presence of 10% palladium-carbon, thus obtaining the objective new erythromycin derivative of the formula [R1 is H or acyl; R2 and R3 are each H, OH, acyloxy, or combined into =O; R4 is H or lower alkyl; Y is formula NR6R7 (R6 and R7 are each H, acyl, lower alkyl, etc.), etc.; Me is methyl] having the above-mentioned advantages.
TSUZUKI KOICHI