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Process for the stereoselective preparation of a - phenylisoserine derivative and its use for the preparation of taxane derivatives

机译:立体选择性制备α-苯基异丝氨酸衍生物的方法及其在制备紫杉烷衍生物中的用途

摘要

This invention relates to a method of stereoselective preparation of a derivative of -phenylisoserine of formula (I) by the action of an N- carbonyl-benzylimine of formula (II) on an optically active amide of a protected hydroxyacetic acid of formula (III), followed by hydrolysis of the product obtained. In formula (I), (II) or (III), R is an optionally substituted phenyl radical or R.sub.1 --O, Ar is an optionally substituted aryl radical and G.sub.1 is a hydroxy function protection grouping. The product of formula (I) is particularly useful in preparing taxol and Taxotere which have remarkable antitumor properties. ##STR1##
机译:本发明涉及一种通过式(II)的N-羰基-苄基亚胺在被保护的式(III)的羟基乙酸的光学活性酰胺上的立体选择性地制备式(I)的-苯基异丝氨酸衍生物的方法。 ,然后水解所得产物。在式(I),(II)或(III)中,R为任选取代的苯基或R 1 -O,Ar为任选取代的芳基,G 1为羟基官能保护基团。式(I)的产物特别用于制备具有显着的抗肿瘤特性的紫杉酚和紫杉醇。 ## STR1 ##

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