A NEW APPROACH TO THYMIDYLATE SYNTHETASE INHIBITORS

被引：8

作者：

FARINA, V

FIRESTONE, RA

机构：

[1] Bristol-Myers Squibb, Pharmaceutical Research Institute, Wallingford, CT 06492-7660

来源：

TETRAHEDRON | 1993年 / 49卷 / 04期

关键词：

D O I：

10.1016/S0040-4020(01)80324-0

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A new approach to the design of thymidylate synthase inhibitors for cancer chemotherapy is described. Several uracil and 2-deoxyuridine derivatives bearing vinylsulfoxide moieties at C-5 were prepared. The two methods described involve a Pd-catalyzed coupling utilizing suitably substituted organostannanes, and a stepwise route involving the regioselective addition of sulfenyl chlorides to 5-vinyluracil and its corresponding nucleosides.

引用

页码：803 / 810

页数：8

共 15 条

[1] CHEMISTRY OF HETEROARYLPHOSPHORUS COMPOUNDS .2. IMPORTANCE OF INDUCTIVE EFFECTS OF PRE-EQUILIBRIA IN ALKALINE-HYDROLYSIS OF HETEROARYLPHOSPHONIUM SALTS - PHOSPHORUS-31 NUCLEAR MAGNETIC-RESONANCE STUDIES [J].