Process for preparation of erythromycin compounds
AssigneesUbe Industries, Ltd., Chugai Seikyaku Kabushiki Kaisha
InventorsHiroyuki Miyata, Akira Takama, Yasuhito Yamamoto, Kikuo Ataka
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Abstract
The present invention is to provide a process for producing a 2′-O-acetyl-4″-O-formyl-8,9-anhydroerythromycin A 6,9-hemiketal compound 4, and it provide a process for producing an erythromycin compound which comprises reacting a formylating agent with a 2′-O-acetylerythromycin A compound 2 to obtain 2′-O-acetyl-4″-O-formylerythromycin A compound 3, then, acting an acid on Compound 3 to subject to hemiketalation, and then adding an aqueous basic solution in an aqueous solution to precipitate Compound 4 as free crystals.
Claims14
A process for producing an erythromycin compound which is a 2′-O-acetyl-4″-O-formyl-8,9-anhydroerythromycin A 6,9-hemiketal compound 4 represented by the formula (4):
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- wherein R1 and R2 each independently represent a lower alkyl group,
- which comprises reacting a 2′-O-acetylerythromycin A compound 2 represented by the formula (2):
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- wherein R1 and R2 have the same meanings as defined above,
- with a formylating agent to obtain a 2′-O-acetyl-4″-O-formylerythromycin A compound 3 represented by the formula (3):
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- wherein R1 and R2 have the same meanings as defined above,
- then, reacting Compound 3 with an acid to subject to hemiketalation, and adding an aqueous basic solution in an aqueous solution to precipitate Compound 4 as free crystals.
A process for isolating and purifying a 2′-Q-acetyl-4″-O-formyl-8,9-anhydroerythromycin A 6,9-hemiketal 5 compound represented by the formula (4):
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- wherein R1 and R2each independently represent a lower alkyl group,
- wherein the preparation process comprises adding a basic solution to an aqueous solution containing the compound and impurities to precipitate the compound from the aqueous solution as free crystals.
Dependencies are inferred from the claim text.