合成路线图解说明: Oxidation of 10-deacetylbaccatin III (I) by means of cupric acetate yielded diketone (II), in equilibrium with the retroaldol product (III). Subsequent reduction employing NaBH4 and CeCl3 produced the seco-taxane (IV) as the major reaction product. Selective protection of the 7 and 9 hydroxyl groups was achieved by treatment with chlorotriethylsilane and imidazole. The resultant 7,9-disilylated derivative (V) was then acylated by the oxazolidinecarboxylic acid (VI) to furnish, after acidic hydrolysis, the title C-seco taxane derivative. |