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[摘要]:A method has been developed for the methylation of the C3' amide of taxol C and paclitaxel. Taxol C and paclitaxel were sequentially silylated at the 2', 7, and 1-hydroxyl groups with tert-butyldimethylsilyl chloride, triethylsilyl chloride, and dimethylsilyl chloride, resp. Subsequent reaction with potassium tert-butoxide and Me iodide provided the corresponding N-methylated taxane derivs. Removal of the silyl protecting groups furnished N-methyltaxol C and N-methylpaclitaxel. |
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