申请人:Rhone-Poulenc Rorer, S.A.
公开号:US05811550A1
公开(公告)日:1998-09-22
Method for the preparation of 1,3-oxazolidin 5-carboxylic acid having the general formula (I) ##STR1## from a product having the general formula (II) ##STR2## In the general formulas (I) and (II), Ar is an aryl radical, R.sub.1 is a benzoyl radical or a radical R.sub.2 --O--CO-- wherein R.sub.2 is an alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl or heterocyclyl radical, Ph is an optionally substituted phenyl radical, X is the residue of an optically active organic base or an alkoxy radical optionally substituted by a phenyl radical. The acids of formulas (I) and (II) are particularly useful in preparing taxol, Taxotere or analogs thereof which have remarkable antitumor and antileukemia properties.
公式(I)的1,3-噁唑烷-5-羧酸的制备方法,其通式为 ##STR1## 从通式(II)的产物中制备。##STR2## 在通式(I)和(II)中,Ar是芳基基团,R.sub.1是苯甲酰基团或R.sub.2-O-CO-基团,其中R.sub.2是烷基,烯基,炔基,环烷基,环烯基,双环烷基,苯基或杂环基团,Ph是可选取代的苯基团,X是光学活性有机碱或可选取代苯基团的烷氧基的残基。公式(I)和(II)的酸在制备紫杉醇,紫杉醇二倍体或类似物方面特别有用,具有显著的抗肿瘤和抗白血病特性。