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Process for synthesizing cyclic depsipeptides

机译:合成环状二肽的方法

摘要

A process for the total synthesis of a cyclic peptide useful as an antifungal drug is disclosed as are novel compounds prepared by the method. The process for synthesizing a cyclic peptide represented by the following formula (I): CHEM wherein X1, X2, X4 and X7 are independently N-methyl- alpha -amino acid or alpha -hydroxy acid, provided that at least one of X1, X2, X4 and X7 is a alpha -hydroxy acid; X3, X6 and X8 are independently alpha -amino acid; X5 is a cyclic amino acid; X9 is a N-methyl- alpha -amino acid or alpha -hydroxy acid substituted by a hydroxy group; and the dotted lines represent intramolecular hydrogen bonds; comprises cyclizing a corresponding linear peptide between X5 and X6 via peptide bond, and a novel compound represented by the formula (I).
机译:公开了用于抗真菌药物的环肽的全合成方法,以及通过该方法制备的新型化合物。合成由下式(I)表示的环肽的方法:<化学式>其中X1,X2,X4和X7独立地是N-甲基-α-氨基酸或α-羟基酸,条件是X1中的至少一个,X 2,X 4和X 7是α-羟基酸; X3,X6和X8独立地是α-氨基酸; X5是环状氨基酸; X9是被羟基取代的N-甲基-α-氨基酸或α-羟基酸。虚线表示分子内氢键。包括通过肽键将相应的线性肽在X5和X6之间环化,以及由式(I)表示的新型化合物。

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