SYNTHESIS AND BIOLOGICAL-ACTIVITY OF PARASUBSTITUTED 3'-PHENYL DOCETAXEL ANALOGS

被引：6

作者：

BOURZAT, JD ^{[1
]}

LAVELLE, F ^{[1
]}

COMMERCON, A ^{[1
]}

机构：

[1] RHONE POULENC RORER SA,CTR RECH VITRY ALFORTVILLE,F-94403 VITRY,FRANCE

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1995年 / 5卷 / 08期

关键词：

D O I：

10.1016/0960-894X(95)00118-D

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

An expedient route for semisynthetic para-modified 3'-phenyl docetaxel analogs is described using the initial regioselective iodination of the oxazolidinecarboxylate 3. Palladium catalyzed coupling reactions of the iodo intermediate 4 with alkenyl and aryl boronic acids and alkynes led after alkaline hydrolysis to a series of N,O-protected para-substituted phenylisoserines 6. Coupling with 10-deacetyl-7,10-O-diTroc-baccatin III followed by standard deprotections and acylation afforded the title analogs.

引用

页码：809 / 814

页数：6

共 29 条

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