Reductive alkylation of glycopeptide antibiotics

Details Reductive alkylation of glycopeptide antibiotics Reductive alkylation of glycopeptide antibiotics

A - Human Necessities

61

K

A61K 38/00 (2006.01) A61K 38/14 (2006.01) C07K 9/00 (2006.01)

Patent

CA 2272240

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.

La présente invention concerne des procédés améliorés d'alkylation réductrice d'antibiotiques glycopeptidiques. L'amélioration consiste à fournir une source de cuivre, ce qui permet d'obtenir la production initiale d'un complexe de cuivre de l'antibiotique glycopeptidique. L'alkylation réductrice de ce complexe favorise une alkylation sélective par régions et des rendements accrus. La présente invention concerne également des complexes de cuivre de matières de départ de l'antibiotique glycopeptidique et des produits alkylés.

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