| 摘要 |
<p>Disclosed is a method of preparing a thiohydrazide compound a formula (II) from a hydrazide starting compound of formula (I). The method comprises reacting the starting compound of formula (I) with a thionylating reagent. The thiohydrazide of formula (II) can be reacted with compounds of the formula Z-C(O)-Y-C(O)-z or HO-C(O)-Y-C(O)-OH and a carboxylic acid activating agent to produce compound of formula III which enhance the anti-cancer activity of taxol and analogs thereof. The variables R1, R2,R5, R10, Y and Z are as defined in the claims.</p> |
