FIELD: chemistry.
SUBSTANCE: invention relates to a method for synthesis of cyclic depsipeptides, particularly emodepside. Disclosed is a method for the synthesis of cyclic depsipeptides of general formula (I) on an industrial scale from depsipeptides of general formula (II), where B is a protective group of an amine group and A is a protective group of a carboxylic acid group, wherein the method comprises the steps of: removing the protective group of an amine group which is protected by group B, thereby obtaining an unprotected amine group; removing protective group of carboxylic acid, which is protected by group A, thus obtaining unprotected group of carboxylic acid; condensation of an unprotected amine group and an unprotected carboxylic acid group with a binding agent, wherein the binding agent is added slowly, preferably drop by drop, to the reaction solution, thus obtaining cyclic depsipeptide (I), wherein R1-R12 are defined in the claims, where the binding agent is T3P® (propylphosphonic acid anhydride, 2,4,6-tripropyl-1,3,5,2,4,6-trioxatriphosphorinane-2,4,6- trioxide, PPACA).
EFFECT: method for synthesis of cyclic depsipeptides is disclosed.
31 cl, 9 dwg, 6 ex
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Authors
Dates
2024-04-09—Published
2018-11-06—Filed