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2-取代-3-芳基-4-噻唑啉(硫)酮衍生物的合成、晶体结构和生物活性
引用本文:孙小军,董卫莉,赵卫光,李正名.2-取代-3-芳基-4-噻唑啉(硫)酮衍生物的合成、晶体结构和生物活性[J].有机化学,2007,27(11):1374-1380.
作者姓名:孙小军  董卫莉  赵卫光  李正名
作者单位:1. 南开大学元素有机化学国家重点实验室,农药国家工程研究中心,天津,300071;淮阴师范学院化学系,淮安,223001
2. 南开大学元素有机化学国家重点实验室,农药国家工程研究中心,天津,300071
基金项目:国家自然科学青年基金(No.20202003),“973”(No.2003CB114406)资助项目
摘    要:从2-取代-3-芳基-4-噻唑啉酮(4a4e5)合成了三个系列新型噻唑啉酮衍生物, 即5-芳基亚甲基-4-噻唑啉酮(6a6j), 4-噻唑硫酮(7a7e8)和4-氰基亚胺基噻唑烷(11a11e12). 中间体4a4e5由醛、胺和巯基乙酸缩合得到. 所有化合物的结构均经元素分析和1H NMR确证, 并且采用X射线单晶衍射分析方法测定了化合物4b的结构. 初步生物活性试验结果表明, 部分标题化合物具有一定的杀菌活性和促进黄瓜子叶生根活性.

关 键 词:4-噻唑啉酮  4-氰基亚胺基噻唑烷  合成  晶体结构  生物活性
收稿时间:2006-12-25
修稿时间:2007-04-09

Synthesis, Crystal Structure and Biological Activities of 2-Substituted- 3-aryl-4-thiazolidinone(thiazolidinethione) Derivatives
SUN, Xiao-Jun,DONG, Wei-Li,ZHAO, Wei-Guang,LI, Zheng-Ming.Synthesis, Crystal Structure and Biological Activities of 2-Substituted- 3-aryl-4-thiazolidinone(thiazolidinethione) Derivatives[J].Chinese Journal of Organic Chemistry,2007,27(11):1374-1380.
Authors:SUN  Xiao-Jun  DONG  Wei-Li  ZHAO  Wei-Guang  LI  Zheng-Ming
Institution:1 National Key Laboratory of Elemento-Organic Chemistry, Pesticide National Engineering Research Center, Nankai University, Tianjin 300071;2. Department of Chemistry, Huaiyin Teachers College, Huaian 223001
Abstract:Three series of new thiazolidinone derivatives, namely 5-arylidene-4-thiazolidinones (6a-6j), 4-thiazolidinethione (7a-7e and 8) and 4-cyanoiminothiazolidine (lla-lle and 12) were synthesized from 2-substituted-3-aryl-4-thiazolidinones (4a-4e and 5). The intermediates 4a-4e and 5 were synthesized by the condensation of aldehyde, amine and mercapto acetic acid. Their structures were characterized by elemental analysis and 1H NMR spectra, and the structure of 4b was determined by X-ray single crystal diffraction method. The preliminary bioassay showed that some title compounds exhibited certain fungicidal activities and promoting cucumber cotyledon root-formation activities.
Keywords:4-thiazolidinone  4-cyanoiminothiazolidine  synthesis  crystal structure  biological activity
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