摘要 |
The process for preparation of docetaxel consists in that the hydroxy! groups at C-7 and C-10 position of 10- deacetolobaccatin III and amino group of (4S,5R)-2- methoxephenyl-4-phenyl-l,3-oxazolidine-5-carboxylic acid are simultaneously protected with allyloxycarbonyl to give 7,10- diallyloxycarbonyl-10-deacetylbaccatin III (VI) and (4S,5R)-N- allyloxycarbonyl-2-(4-metoxyphenyl)-4-phenyloxazolidine-5- carboxylic acid (IV), respectively, said groups after esterification are removed upon one technological operation, whereas the synthesis is finalized by the introduction of tert-butyloxycarbonyl group onto amino group of (2R,3S)-3-phenylisoserine. |