Preparation method of peg-maleimide derivatives
AssigneeSunBio Inc.
InventorsKwang Nho, Changmin Hyun, Junghun Lee, Youngkyoung Pak
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Abstract
The present invention relates to novel synthetic methods for PEG-maleimide derivatives, specifically, novel synthetic methods for PEG-maleimide. The final products thereof are useful as a pegylation reagent in the field of bioengineering and the medicinal field or the preparation of medical appliances and by conjugating with certain moieties or specific domains of polysaccharides and biological proteins such as antibodies as a bio-compatible or bio-degradable polymer.
Claims25
A method for preparing a mPEG-maleimide polymer compound, said method comprising:
- reacting an mPEG-maleamic acid derivative in the presence of base, organic solvent and pentafluorophenyl trifluoroacetate, wherein said mPEG-maleamic acid derivative is represented by general formula (I-a)
- mPEG-OCH2CH2—NHCOCH═CHCO2H (Ia)
- thereby forming an mPEG-maleimide polymer compound.
A method for preparing a PEG-(maleimide)2 polymer compound, said method comprising:
- reacting a PEG-maleamic acid derivative in the presence of base, organic solvent and pentafluorophenyl trifluoroacetate, wherein said PEG-maleamic acid derivative is represented by general formula (II-a)
- HO2CCH═CHCONH-PEG-OCH2CH2—NHCOCH═CHCO2H (II-a),
- thereby forming a PEG-(maleimide)2 polymer compound.
A method of preparing a multi-arm PEG-maleimide polymer compound, said method comprising:
- reacting a multi-arm PEG-maleamic acid derivative in the presence of base, organic solvent and pentafluorophenyl trifluoroacetate, wherein said multi-arm PEG-maleamic acid derivative is represented by general formula (III-a)
- R(-PEG-OCH2CH2—NHCOCH═CHCO2H)n (III-a)
- wherein R is central core, n is an integer from 3 to 12 which indicates the number of arms,
- thereby forming a multi-arm PEG-maleimide polymer compound.
A method of preparing a pendant-type multi-arm PEG-maleimide polymer compound, said method comprising:
- reacting a pendant-type multi-arm PEG-maleamic acid derivative in the presence of base, organic solvent and pentafluorophenyl trifluoroacetate, wherein said pendant-type multi-arm PEG-maleamic acid derivative is represented by general formula (IV-a):
- wherein R′ is a hydrogen atom or a lower alkyl group having 1 to 3 carbon, n′ is an integer of 3 to 3000, m is an integer of 1 to 20 which represents the number of arms,
- thereby forming a pendant-type multi-arm PEG-maleimide polymer compound.
Dependencies are inferred from the claim text.