Reductive alkylation of glycopeptide antibiotics

Chemistry: natural resins or derivatives; peptides or proteins; – Peptides of 3 to 100 amino acid residues – Chemical aftertreatment – e.g. – acylation – methylation – etc.

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530317, 530322, 530333, 514 9, A61K 3800, C07K 512

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active

059524669

ABSTRACT:
This invention is concerned with improved processes for reductive alkylation of glycopeptide antibiotics. The improvement residing in providing a source of copper which results in the initial production of a copper complex of the glycopeptide antibiotic. Reductive alkylation of this complex favors regioselective alkylation and increased yields. Copper complexes of the glycopeptide antibiotic starting materials and of the alkylated products are also part of the invention.

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Abstracts of Papers, 210th ACS National Meeting, American Chemical Society, Chicago, Illinois, (Aug. 1995).

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