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通过关环复分解反应合成新型双环氟化尿嘧啶及其生物学评价

Synthesis and biological evaluation of new bicyclic fluorinated uracils through ring-closing metathesis.

作者信息

Fustero Santos, Catalan Silvia, Piera Julio, Sanz-Cervera Juan F, Fernandez Begoña, Aceña José Luis

机构信息

Departamento de Química Organica, Universidad de Valencia, E-46100 Burjassot, Spain. Spain

出版信息

J Org Chem. 2006 May 12;71(10):4010-3. doi: 10.1021/jo0601765.

Abstract

Two families of bicyclic fluorinated uracils have been prepared starting from a gem-difluorinated unsaturated nitrile, by means of a ring-closing metathesis reaction to form the new ring, which is fused at the C-5/C-6 or N-1/C-6 positions of the uracil moiety. The selective formation of olefin regioisomers in the metathesis process can be controlled according to the reaction conditions (catalyst, solvent, and temperature). The acaricidal activities of the resulting compounds have also been investigated.

摘要

从偕二氟不饱和腈出发,通过关环复分解反应形成新环,制备了两类双环氟化尿嘧啶,该新环与尿嘧啶部分的C-5/C-6或N-1/C-6位稠合。复分解过程中烯烃区域异构体的选择性形成可根据反应条件(催化剂、溶剂和温度)进行控制。还研究了所得化合物的杀螨活性。

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