Processes for the preparation of docetaxel and paclitaxel or analogs from 9-dihydro-13-acetylbaccatin III via key intermediates (4), (5), (6), (6'), (8) and (8') or via intermediate (12) as well as processes for the preparation of said intermediates are disclosed. Said processes involve, in particular, oxidation of the hydroxy group at C-10, reaction with side chain precursors and intramolecular isomerisation of the oxo at C-10 to produce the 9-oxo isomer. Paclitaxel and docetaxel are useful in the treatment of cancer. Formulae (I), (II), (III).
从9-二氢-13-乙酰基
紫杉醇III经过关键中间体(4)、(5)、(6)、(6')、(8)和(8')或经过中间体(12)制备
紫杉醇和多西
紫杉醇或类似物的过程以及制备所述中间体的过程被披露。这些过程涉及特别是氧化C-10处的羟基、与侧链前体反应以及C-10处的酮的分子内异构化以产生9-酮异构体。
紫杉醇和多西
紫杉醇在癌症治疗中很有用。公式(I)、(II)、(III)。