期刊论文

Shi, De-Qing

英文

PHOSPHORUS SULFUR AND SILICON AND THE RELATED ELEMENTS

1042-6507

2008

183

12

3156-3165

10.1080/10426500802070270

Received 21 February 2008; accepted 20 March 2008. The project was sponsored by the Natural Science Foundation of china (No. 20302002) and the Scientific Research Foundation for the Returned Overseas Chinese Scholars, State Education Ministry (No. [2007] 1108). Address correspondence to D.-Q. Shi, College of Chemistry, Central China Normal University, Wuhan 430079, Hubei, P. R. China. E-mail: chshidq@mail.ccnu.edu.cn

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An important building block, diethyl [(5-amino-4-cyano-3-methylsulfanyl-pyrazol-1-yl)-(4-fluorophenyl)methyl] phosphonate (3) was efficiently synthesized via the condensation of 1-hydrazino-1-(4-fluorophenyl)methyl phosphonate (1) with 2-[bis(methylthio)methylene]malononitrile (2).3 reacted with triethyl orthoformate to afford diethyl [(4-cyano-5-ethoxymethyleneamino-3-methylsulfanyl-pyrazol-1-yl)-(4-fluorophenyl)methyl] phosphonate (4), which reacted with various acyl hydrazines in refluxing 2-methoxyethanol to provide the target compounds (5) in good yields directly. The results of prelimina...