Method of producing epirubicin and novel production intermediate thereof
AssigneeMeiji Seika Pharma Co., Ltd.
InventorsKenichiro Mori, Takuto Umezu, Takahisa Maruyama, Sojiro Shiokawa
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Abstract
According to the present invention, it is possible to efficiently remove 13-dihydroepi-daunorubicin and 4′-epi-feudomycin, which are typical impurities possibly contained in 4′-epi-daunorubicin as a starting material, by using an organic acid salt of 4′-epi-daunorubicin or a hydrate or solvate thereof as a novel production intermediate, thus making it possible to produce high-purity epirubicin.
Claims9
A method of producing an organic acid salt of 4′-epi-daunorubicin or a hydrate or solvate thereof, comprising a step of mixing 4′-epi-daunorubicin of the following formula (1):
- with an organic acid in a solvent to form an organic acid salt of 4′-epi-daunorubicin of the following formula (2):
- wherein HA represents an organic acid,
- or a hydrate or solvate thereof,
- wherein the organic acid salt of the 4′-epi-daunorubicin is selected from the group consisting of an oxalate, a benzenesulfonate and a p-toluenesulfonate.
An organic acid salt of 4′-epi-daunorubicin of the following formula (4):
- wherein HA represents oxalic acid, benzenesulfonic acid, or p-toluenesulfonic acid, or a hydrate or solvate thereof.
An organic acid salt of 4′-epi-daunorubicin or a hydrate or solvate thereof, having a HPLC purity of 90% or more, wherein the organic acid salt of the 4′-epi-daunorubicin is selected from the group consisting of an oxalate, a benzenesulfonate and a p-toluenesulfonate.
Dependencies are inferred from the claim text.