A synthetic route of water-soluble docetaxel derivative (Ⅰ) was designed. 7, 10-Oxo- dibenzyloxy oxygen acyl-docetaxel (Ⅴ) was obtained through esterification, condensation and selective deprotection of 10-deacetylbaccatin III (Ⅱ) as the starting material. This key intermediate was further reacted with an amino acid, and followed by hydrogenolysis in the presence of palladium on carbon to obtain the target docetaxel derivative (Ⅰ). The structure of product was characterized by means of 1HNMR, 13CNMR and HRMS. The synthetic route was benefited from simple operation, overall yield of 64.1% and purity of over 99% (HPLC).