Preparation method of histone deacetylase inhibitor FK228

A technology of FK228 and condensing agent, which is applied in the direction of chemical instruments and methods, cyclic peptides, etc., can solve the problems of limiting the preparation of FK228, and achieve the effects of avoiding product deterioration, high yield, and simple reaction conditions
CN101935337AInactive Publication Date: 2011-01-05无锡好芳德药业有限公司
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
无锡好芳德药业有限公司
Publication Date
2011-01-05
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses a new method for preparing depsipeptide FK228, comprising the following steps of: firstly forming annular polypeptide in a ring-closing way through the condensation reaction of an amido bond; and then forming the coupling of sulfide-sulfide bonds through radical reaction catalyzed by iodine by using a mixed solution of methylene dichloride and methanol as a solvent so as to synthesize the FK228. The preparation method of the FK228 has the advantages of easy operation and low cost, primarily discloses a process for preparing gram-grade FK228, greatly enhances the yield compared with past literatures and patents and provides new selection for the preparation and the production of the FK228.
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Description

technical field

[0001] The invention relates to a method for preparing medicine, in particular to a method for preparing FK228. Background technique

[0002] Desipeptide FK228 (Dep sipep tide FK228) is a bicyclic tetrapeptide isolated from the broth medium of Chlorobacter violaceum. In addition to forming a bicyclic structure through disulfide bonds and ester bonds, its amino acid sequence also has the characteristics of alternately connecting through amide bonds and ester bonds. In addition, FK228 contains both common L-valine, D-valine, D-cysteine ​​and a special amino acid (Z)-2-amino-2-butenoic acid with a double bond And mercapto-containing chain structure unit (3S, 4E)-3-hydroxyl-7-mercapto-4-heptenoic acid. In vitro experiments on human cancer cell lines and in vivo experiments on human tumor grafts and mouse tumors, FK228 showed good anti-tumor activity, and was listed by the US Food and Drug Administration (FDA) in October 2004. "Express Approval" channel. The c...

Claims

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