摘要
以氢亚磷酸酯为原料合成了次亚甲基双膦酸四乙基酯,又通过加成和消除反应合成了亚乙烯基双膦酸四乙基酯,再与2-胺基-5-巯基-1,3,4-噻二唑Michael反应,根据反应物物质的量不同,合成了不同的目标化合物,并探讨了其与—NH2和—HS的反应选择性,其结构均经ESI-MS、IR、1HNMR和13CNMR测试手段所确认,其生物活性在进一步的研究中。
The tetraethyl methylene biphosphonate was synthe- sized by the reaction of diethylpho-sphite with sodium ethox- ide and CH2Cl2. The tetraethyl ethenylidene-1,1-bisphospho- hate was obtained from tetraethyl methylene biphosphonate with paraformaldehyde and other compounds,via addition and reduction reaction. The various target compounds were synthe- sized by the reaction of 2-amino-5-mercapto-1, 3,4-thia- diazole with the tetraethyl ethenylidene-1,1-bisphosphonate via a facile Michel addition reaction, according to the reactant amount of substance. The selective reactivity of Michael addi- tion reaction between --SH or --NH2 group in the same sub- strate and the tetraethyl ethenylidene-1, 1-bisphosphonate were further discussed in the paper. The strures of target com- pounds were confirmed by ESI-MS, IR, 1HNMR and 13 CNMR and the biological activities are further investigated.
出处
《化学试剂》
CAS
CSCD
北大核心
2013年第6期573-576,共4页
Chemical Reagents
关键词
亚乙烯基双膦酸酯
1
3
4-噻二唑
反应选择性
ethenylidene-1,1 -bisphosphonate
1,3,4-thiadi- azole
selective reactivity
