Erythromycin derivative having novel crystal structures and processes for their production
AssigneeChugai Seiyaku Kabushiki Kaisha
InventorsAkira Hiraide, Kaichiro Koyama, Hitoshi Shimizu, Kaname Tsuzaki
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Abstract
The present invention provides an E-type crystal of N-demethyl-N-isopropyl-12-methoxy-11-oxo-8,9-anhydroerythromycin A-6,9-hemiacetal fumarate having strong diffraction peaks at diffraction angles (2θ) of 5.6° and 10.4° as measured by powder X-ray diffractometry, which is prepared by treating a C-type crystal of the compound in a mixed solvent of ethyl acetate and water at 20° C. to 40° C., and a D-type crystal prepared via the E-type crystal. These crystals have a reduced content of residual solvent and high suitability for formulation.
Claims12
An E-type crystal of a fumarate salt of the compound represented by formula (I):
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- wherein said e-type crystal has strong x-ray diffraction peaks at diffraction angles (2θ) of 5.6° and 10.4° as measured by x-ray diffractometry with Cu—Kα radiation.
A method for preparing an E-type crystal of a fumarate salt of the compound represented by formula (I):
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- which comprises treating a C-type crystal of a fumarate salt of compound (I) in a mixed solvent of ethyl acetate and water at 20° C. to 40° C., wherein said E-type crystal has strong X-ray diffraction peaks at diffraction angles (2θ) of 5.6° and 10.4° as measured by X-ray diffractometry with Cu—Kα radiation.
A D-type crystal of a fumarate salt of the compound represented by formula (I):
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- which is obtainable via an E-type crystal of a fumarate salt of compound (I) having strong X-ray diffraction peaks at diffraction angles (2θ) of 5.6° and 10.4° as measured by X-ray diffractometry with Cu—Kα radiation.
A method for preparing a D-type crystal of a fumarate salt of the compound represented by formula (I):
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- which comprises obtaining the D-type crystal via an E-type crystal of a fumarate salt of compound (I) having strong X-ray diffraction peaks at diffraction angles (2θ) of 5.6° and 10.4° as measured by X-ray diffractometry with Cu—Kα radiation.
Dependencies are inferred from the claim text.