Method for preparing fatty acyl cyclic depsipeptide compounds by solid-phase synthesis

The technology of a fatty acyl cyclic ester and a synthesis method is applied in the field of solid-phase synthesis to prepare fatty acyl cyclic ester peptide compounds, which can solve the problems of incomplete esterification of fatty acyl cyclic ester peptides, difficult cyclization and the like, and achieves high synthetic yield, simple method effect
CN102020703AInactive Publication Date: 2011-04-20NORTHWESTERN POLYTECHNICAL UNIV
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
NORTHWESTERN POLYTECHNICAL UNIV
Publication Date
2011-04-20
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention relates to a method for preparing fatty acyl cyclic depsipeptide compounds by solid-phase synthesis, which comprises the following steps of: adding amino resin from which fluorenl methoxy carbonyl (Fmoc) is removed, Fmoc-Asp-Odmab, an active agent and straight-chain polypeptide serving as a shrinking agent into a reactor; adding a detritylation reagent into the reactor to immerse a reactant, performing a reaction, and connecting side chain amino acid by an active ester method to obtain a protected cyclization precursor compound; adding a fluorenl methoxy carbonyl removing reagent into the resin for reacting, and washing the resin by using N,N-dimethylformamide; and adding a cyclization agent into the resin to obtain cyclic decapeptide products. By the method, the compounds and analogues thereof are synthesized successfully. The method is simple and high in synthesis yield, and is suitable for synthesizing cyclic depsipeptide with the similar structure.
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Description

technical field

[0001] The invention relates to a method for solid-phase synthesis of aliphatic acyl-cyclic ester peptide compounds, in particular to methods for selection of starting amino acids, esterification reaction and cyclization reaction. Background technique

[0002] In recent years, the problem of antibiotic resistance has become more and more serious, and the need for new antibiotics has become more and more urgent. Antimicrobial peptide antibiotics are a large class of non-specific immune compounds with significant anti-infective activity. Among them, the cyclic lipopeptide antimicrobial peptides are the most eye-catching. As in September 2003, Daptomyhcin for injection approved by the U.S. FDA is exactly a kind of cyclic lipopeptide antibiotics. Its cyclic lipopeptide part is composed of ten It consists of two amino acids with a n-decanoic acid in the side chain. It can be used to treat skin and soft tissue infections and has good results against methicillin-r...

Claims

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