METHOD OF PREPARING SUBSTITUTED TETRACYCLINE WITH TRANSITION METAL-BASED CHEMISTRIES

摘要

PROBLEM TO BE SOLVED: To provide a method of synthesizing a novel substituted tetracycline compound; and to provide the compound.

SOLUTION: A 7- and/or 9-substituted tetracycline compound is prepared by: bringing a reactive tetracycline-based precursor compound selected from a tetracycline diazonium salt and a halogenated derivative of tetracycline, into contact with a reactive organic substituent, e.g., alkenes comprising π bond, substituted alkenes, vinyl monomers, aromatics and heteroaromatic compounds, in the presence of a transition metal catalyst, such as palladium chloride and copper chloride; and reacting them with each other.

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