Methods and compositions for converting taxane amides to...

Details Methods and compositions for converting taxane amides to... Methods and compositions for converting taxane amides to...

C - Chemistry, Metallurgy

07

D

C07D 305/14 (2006.01)

Patent

CA 2741496

A method for forming a taxane from a compound represented by the following formula: (see above formula) wherein: R2 is H, Ac or a protecting group; R3 is H, xylosyl or protecting group; R4 is H or protecting group; R N is H or an alkyl group; and X is a deprotonated sulfuric acid or deprotonated sulfur containing acid, a deprotonated nitric acid or other nitrogen containing acid, a deprotonated carboxylic acid, except trifluoro acetic acid, a deprotonated phosphoric acid or any phosphorus containing acid, a deprotonated tartaric acid, a deprotonated p-toluene sulfonic acid, or a deprotonated picric acid, the method comprising benzoylating the compound with a benzoylation solution comprising a benzoylating agent and a buffer such that the pH of the benzoylation solution is about 4 to about 6.

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