A CHEMOSELECTIVE APPROACH TO FUNCTIONALIZE THE C-10 POSITION OF 10-DEACETYLBACCATIN-III - SYNTHESIS AND BIOLOGICAL PROPERTIES OF NOVEL C-10 TAXOL(R) ANALOGS

被引：39

作者：

KANT, J

OKEEFFE, WS

CHEN, SH

FARINA, V

FAIRCHILD, C

JOHNSTON, K

KADOW, JF

LONG, BH

VYAS, D

机构：

[1] BRISTOL MYERS SQUIBB CO,PHARMACEUT RES INST,WALLINGFORD,CT 06492

[2] BRISTOL MYERS SQUIBB CO,PHARMACEUT RES INST,PRINCETON,NJ 08543

来源：

TETRAHEDRON LETTERS | 1994年 / 35卷 / 31期

关键词：

D O I：

10.1016/S0040-4039(00)77242-X

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A chemoselective approach to functionalize the C-10 position of 10-deacetyl baccatin III, a key intermediate for the semi-synthesis of paclitaxel, is described. The chemistry provides an easy access to a variety of C-10 hydroxyl derivatives, such as, ethers, esters, carbonates, carbamates, and sulfonates under mild conditions. The C-10 modified baccatin derivatives were further employed in the synthesis of never biologically active Taxol(R) analogues.

引用

页码：5543 / 5546

页数：4

共 18 条

[1]

BOURZAT JD, 1993, Patent No. 524093

[2] SYNTHESIS OF 10-DEACETOXYTAXOL AND 10-DEOXYTAXOTERE [J].