Microwave-assisted, one-pot syntheses and fungicidal activity of polyfluorinated 2-benzylthiobenzothiazoles

被引：167

作者：

Huang, Wei ^{[1
]}

Yang, Guang-Fu ^{[1
]}

机构：

[1] Cent China Normal Univ, Coll Chem, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2006年 / 14卷 / 24期

基金：

中国国家自然科学基金;

关键词：

benzothiazole; one-pot synthesis; microwave irradiation; fungicidal activity;

D O I：

10.1016/j.bmc.2006.09.016

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Polyfluorinated 2-benzylthiobenzothiazoles 3a-1 are prepared via a microwave-assisted, one-pot procedure. The advantages, such as good to excellent yields, shorter reaction time (14-21 min), readily available starting material, and simple purification procedure, distinguish the present protocol from other existing methods used for the synthesis of 2-benzylthiobenzothiazoles. Bioassay indicated that most of the compounds showed significant fungicidal activity against Rhizoctonia solani, Botrytis cinereapers, and Dothiorella gregaria at a dosage of 50 mu g/mL. Interestingly, compared to the control of commercial fungicide, triadimefon, compound 3c exhibited much higher activities against R. solani, B. cinereapers, and D. gregaria, which showed that the polyfluorinated 2-benzylthiobenzothiazoles can be used as lead compound for developing novel fungicides. (c) 2006 Elsevier Ltd. All rights reserved.

引用

页码：8280 / 8285

页数：6

共 21 条

[1] Sceptrin as a potential biosynthetic precursor to complex pyrrole - Pyrrole-imidazole alkaloids: The total synthesis of ageliferin [J].